Accepted Manuscript

Pharmaceutical significance of Eudragit: A review

Ch. Niranjan Patra, Richa Priya, Suryakanta Swain, Goutam Kumar Jena, Kahnu
Charan Panigrahi, Debashish Ghose

PII: S2314-7245(16)30127-3
DOI: 10.1016/j.fjps.2017.02.001
Reference: FJPS 26

To appear in: Future Journal of Pharmaceutical sciences

Received Date: 19 September 2016

Accepted Date: 13 February 2017

Please cite this article as: Patra CN, Priya R, Swain S, Kumar Jena G, Panigrahi KC, Ghose D,
Pharmaceutical significance of Eudragit: A review, Future Journal of Pharmaceutical sciences (2017),
doi: 10.1016/j.fjps.2017.02.001.

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Pharmaceutical Significance of Eudragit: A Review

Ch.Niranjan Patra1*, Richa Priya1, , Suryakanta Swain2, Goutam Kumar Jena1 , Kahnu Charan
Panigrahi1 and Debashish Ghose1

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1
Roland Institute of Pharmaceutical Sciences, Berhampur-760010, India.
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SIMS College of pharmacy, Guntur, India.

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Address for correspondence:

Dr. Ch.Niranjan Patra

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Professor,
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Roland Institute of Pharmaceutical Sciences,

Berhampur-760010,

Ganjam, Odisha, INDIA.

E mail: drniranjanrips@gmail.com
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Pharmaceutical Significance of Eudragit: A Review

INTRODUCTION

The Eudragit® range of polymers, like the versatile acrylic material Plexiglas (introduced

in 1933), grew out of Dr. Rohm’s deep knowledge of acrylic acid and its derivatives. In the year

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1954 first two polymers Eudragit L and Eudragit S for enteric coating were launched. It offered

a synthetic polymer for film-coating of improved quality than materials such as sugar and

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shellac. Eudragit based products for rapidly disintegrating and sustained release coatings were

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added during the 1960s, expanding the widening potential applications considerably. The

introduction of aqueous polymer dispersion forms of Eudragit in 1972 was a major milestone,

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making the process of coating easier, safer, more versatile and economical. With the
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development of various grades of Eudragit, it became possible to handle many aspects of

formulation development such as film coating, granulation, direct compression, melt extrusion
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and mastery of technologies to engineer immediate or sustained release, as well as GI targeting,

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enteric coatings, pulsed release and transdermal formulations. Hence Eudragit a versatile

polymer for drug delivery was selected for extensive review.

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Polymethacrylates are synthetic cationic and anionic polymers of dimethylaminoethyl

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methacrylates, methacrylic acid, and methacrylic acid esters in varying ratios. Several types are

commercially available and may be obtained as the dry powder, aqueous dispersion, organic
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solution [1]. The most commonly used organic phase used was a (60:40) mixture of acetone and
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propan-2-ol. Polymethacrylates are primarily used as film-coating agents in tablet and capsule

dosage forms. Films of different solubility can be produced by using different polymer grades.

Table 1 outlines the solubility profile of each grade of Eudragit. Broadly polymethacrylates are

used as film former, tablet binder and tablet diluents. Apart from the above applications, recent

studies revealed that polymethacrylates have got widespread applications in formulation vis-à-vis
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taste masking, better permeation across skin, intestinal epithelium and corneal permeation,

dissolution enhancement, bioavailability enhancement, enteric coating, sustain release,

radioprotection, pH dependent release, colon targeting etc. Therefore polymethacrylates play a

pivotal role in formulation and development of different type of dosage forms with versatile

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applications. Hence the objective of the present manuscript is to make a compilation review on

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research publications and patents on various applications of Eudragit.

Polymethacrylates are known with various synonyms such as Acryl-EZE, Acryl-EZE

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MP, Eastacryl 30D; Eudragit; Kollicoat MAE 30 D; Kollicoat MAE 30 DP; polymeric

methacrylates. This present review focused on various grades of Eudragit which is a trademark

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of GmbH & Co.K.G Darmastadt in Germany, first marketed in 1950s. polymerization of acrylic
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& methacrylic acids or their esters was adopted to obtain Eudragit e.g. butyl ester or

dimethylaminoethyl ester. Chemical structure of Eudragit is shown in Figure 1. Eudragit was

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included in USPNF, BP and PhEur. Dry powder polymer forms are stable at temperatures less
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than 30⁰C. Dry powders are stable for at least 3 years if stored in a tightly closed container at less
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than 30⁰C. Dispersions should be stored at temperatures between 5 and 25⁰C and are stable for at

least 18 months. Eudragits are generally regarded as nontoxic and nonirritant materials. A daily
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intake of 2 mg/kg body-weight in humans is regarded as essentially safe. It is included in the

FDA Inactive Ingredients Guide (oral capsules and tablets), nonparenteral medicines licensed in
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the UK, Canadian list of acceptable nonmedicinal ingredients.

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LITERATURE REVIEW

A comprehensive review of literature is discussed in length highlighting their

applications. Research articles reported for each grade are enlisted in tabular form. Some of those

articles are discussed critically with special reference to eudragit.

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Eudragit E100, E12,5 and EPO

In this series there are three different grades of Eudragit vis-a-vis Eudragit E100, E12,5

and EPO. All the three are cationic copolymer based on dimethylaminoethyl methacrylate,

butylmethacrylate and methyl methacrylate. Chemically they are known as poly(butyl

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methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate. They possess a

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molecular weight of approximately (47,000 g/mole), alkali value (180 mg KOH/g of polymer)

and glass transition temperature (480C). They are soluble in gastric pH up to 5.0. Low viscosity,

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high pigment binding capacity, good adhesion and low polymer weight gain are the characteristic

properties of Eudragit E series. They are commonly used in film coating, odor and taste masking,

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moisture and light protection. They differ from each other in terms of their physical appearance.
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Eudragit S100 is available in the form of granules which consists of colourless to yellow tinged

granules with a characteristic amine like odor. Eudragit E 12,5 is available in the form of organic
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solution which is a light yellow liquid of low viscosity, clear to slightly cloudy with
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characteristic odor of solvent. Eudragit EPO is available in the form of powder with a
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characteristic amine like odour.

A current literature review on Eudragit E 100 reveals that it has been used in
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nanoparticles, microparticles, transdermal spray, ophthalmic solution, floating drug delivery

system etc as shown in Table 2. Quinteros et al [2] proposed a novel ophthalmic solution based
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on the ionic complexation between Eudragit E 100 and flurbiprofen. Dispersion of the drug and
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Eudragit complex in 0.9 % w/v sodium chloride (NaCl) increased flurbiprofen release through an

ionic exchange, providing a controlled release and more effective corneal permeation without

any irritation. Paradkar et al [3] formulated clotrimazole transdermal spray using different ratios

of ethanol and acetone and various grades of eudragit and ethyl cellulose. The following
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parameters like viscosity, drying time, stickiness, appearance, integrity on skin and water

washability were evaluated. The desired crieteria was achieved by using Eudragit E100 and

mixture of ethanol and acetone (80:20). The optimized formulation exhibited improved drug

permeation through the rat skin and improved antifungal efficacy as evidenced from higher zone

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of inhibition. Dominguez et al [4], prepared triclosan nanoparticles suspension by the

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emulsification-diffusion by solvent displacement method, using Eudragit® E 100 as polymer.

Triclosan was molecularly dispersed in the nanoparticle batches containing triclosan.

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Nanoparticles exhibited higher permeation compared to solutions and creams. Patil et al [5]

explored the application of Eudragit E 100 as taste masking agent in orally disintegrating tablet

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of tramadol hydrochloride. The results demonstrated successful masking of bitter taste.
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No literature was found for Eudragit 12,5 in pubmed indexed journals. An extensive

review on applications of Eudragit EPO revealed that it can be used in formulations such as solid
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dispersions, orally disintegrating tablets, nanoparticles, nanosuspensions, stabilization of

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liposomes, superior moisture protection for solid dosage forms etc are shown in Table 2. Cantor
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et al [6] explored taste masking potential of Eudragit EPO by formulating orally disintegrating

tablets of clindamycin HCl. Coating of Clindamycin HCl with Eudragit EPO suspension
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subsequent compression into tablet showed improved pediatric and geriatric patient compliance

for clindamycin. Salmani et al [7] investigated solubility and bioavailability enhancement

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potential of orally disintegrating tablet compressed from solid dispersions of atrovastatin with
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Eudragit EPO. Solid dispersions significantly improved the dissolution of atrovastatin. In vivo

study showed. 434 % more bioavailability than plain atrovastatin tablets. Khachane et al [8]

investigated the potential of Eudragit EPO nanoparticles in improving therapeutic efficacy of

meloxicam and compared with conventional meloxicam suspension. Meloxicam loaded eudragit
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EPO nanoparticles were prepared by nanoprecipitation method. Improved anti-inflammatory

activity with lesser ulcerogenicity was observes with optimized nanoparticles. Hasanovic et al

[9] improved physicochemical properties of liposomes by using cationic polymer i.e. chitosan

and Eudragit EPO. 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes were

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prepared by high-pressure homogenisation. Zeta potential and mean particle size revealed that

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the polymeric liposomes are stable. In the presence of the drugs (acyclovir and minoxidil), the

polymeric liposomes still showed constant particle size and zeta potential. Moreover, the coating

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of liposomes with chitosan or Eudragit EPO led to higher skin diffusion for both drugs. The

interaction between the skin (negatively charged surface) and liposomes (positively charged) was

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the probable reason for increased skin diffusion.
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Eudragit L 100 and 12,5

Eudragit L 100 and L 12,5 are anionic copolymers based methacrylic acid and methyl
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methacrylic acid. Both the polymers possess similar molecular weight 1,25,000 g/mol, acid value
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315 mg KOH/g of polymer and glass transition temperature greater than 1500C. Targeted drug
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release area for both the polymer is jejunum and dissolves at pH above 6. They are used for

effective and stable coatings with fast dissolution in the upper bowel, granulation of drug
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substance in powder form for controlled release, site specific drug delivery in intestine etc. The

only difference between these two grades is Eudragit L 100 is available in the form of solid
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powder with a faint characteristic odour whereas Eudragit 12,5 is a organic solution which is
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colourless and clear to slightly cloudy liquid with the characteristic odour of isopropyl alcohol.

A current review on Eudragit L 100 exhibits that it has been used in various formulations

such as microspheres, microsponges, nanoparticles, liposomes, lipotomes, tablets etc for

different applications such as enteric coating, sustain release, insulin permeation, bioavailability
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enhancement etc as shown in Table 3. Li et al [16] filled self nanoemulsifying drug delivery

systems (SNEEDS) of insulin into Eudragit L100 based enteric coated capsules. A pH-dependent

insulin release profile was observed. In healthy fasted rats, administration of SNEDDS produced

a 2.7 and 3.4 fold enhancement in the relative bioavailability and glucose reduction, respectively.

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This study showed enhanced oral absorption and efficacy of insulin. Sareen et al 2014 [17]

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evaluated colon specific drug delivery potential of Eudragit L100 by formulating microponges of

curcumin. Release studies revealed that microsponges prevented the premature release of

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curcumin in upper GIT and specifically released the drug at colonic pH. Microsponges with

Eudragit L 100 can be used as a promising drug delivery system for treatment of ulcerative

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colitis. Hosny et al [18] made a novel approach to overcome barriers for the treatment of
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osteoporosis by formulating enteric-coated alendronate sodium (ALS) nanoliposomes.

Optimized nanoliposome coated with Eudragit L 100 successfully resisted the release of ALS in
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acidic environments and enhanced the bioavailability in rabbits. Wilson et al [19], prepared and
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evaluated sustain release enteric coated tablets of pantoprazole. The prepared tablets were dip
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coated using an enteric coating polymer such as cellulose acetate phthalate and eudragit L100.

The study revealed that the prepared tablets were able to sustain drug release into the intestine.
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The enteric coated pantoprazole tablets significantly reduced ulcer formation. No literature found

for Eudragit 12,5 in pubmed indexed journals.

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Eudragit L 30 D 55 and L 100-55

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Eudragit L 30 D 55 is the aqueous dispersion of anionic polymers with methacrylic acid

as a functional group. It is a low viscosity liquid of white colour with faint characteristic odour.

It is obtainable in the form of aqueous dispersion (30 %) whereas eudragit L 100-55 is an anionic

copolymer based on methacrylic acid and ethyl acrylate. It is a a white powder with a faint
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characteristic odour. Both grades of Eudragit have molecular weight 3,20,000 g/mol, acid value

315 mg KOH/g of polymer and glass transition temperature 1100 C. Targeted drug release area

for both is duodenum and they dissolve at pH of 5.5. Both the polymers are used for effective

and stable coating with fast dissolution in the upper bowel, controlled release, site specific drug

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delivery in intestine etc.

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An up to date literature review on the applications of Eudragit L 30 D 55 polymer

suggests that it has been used in the formulation of microspheres, microparticles, film coated

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tablets, pellets, transdermal film, enteric coating etc with various objectives such as improving

bioavailability, drug release at intestine, sustain release etc as shown in Table 4. Nair et al [23]

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evaluated four different polymers such as Eudragit L-30 D-55, hydroxy propyl methylcellulose
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phthalate, cellulose acetate phthalate and Acryl-EZE® by formulating enteric coated tablets of

esomeprazole magnesium trihydrate. Tablets with 5% weight gain, failed disintegration test in
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0.1 N HCl media. It was observed that 8% w/w enteric coating passed disintegration test.
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Methacrylic polymers (Eudragit L 30 D 55 and Acryl EZE) exhibited better dissolution rate than
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the cellulose polymers. Naseem et al [24] designed transdermal films of tenoxicam with Eudragit

L 30D55 along with permeation enhancers like polyethylene glycol (PEG) and propylene glycol
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(PG). A drag effect was observed due to interaction between tenoxicam and Eudragit L30D-55

leading to a delay of the tenoxicam release. Bendas et al [25] attempted extrusion-spheronization

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followed by spray coating for leaky enteric-coated pellets of ranitidine HCl. Pellets were
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prepared using Eudragit L 30 D-55, combined with soluble lactose, PEG 8000 and surfactants

(span 60 (hydrophobic) or tween 80 (hydrophilic). Leaky enteric coated pellets allowed the

release of some amount of drug in gastric fluid.

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Similarly an extensive up to date review on the polymer Eudragit L100-55 suggests that

this can be used in the formulations for various applications such as pH responsive drug release,

taste masking, drug release at intestine, radioprotection etc as shown in Table 4. Lotikar et al

[26] designed multiparticulate dosage form of ketoprofen by extrusion and spheronization

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technique. It was based on pH-responsive dual pulse release concept. Pellets were coated with

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pH sensitive Eudragit L 100-55 and Eudragit S 100 for site-specific drug release with lag time.

The dual pulse release after a lag time of 2 and 5 h was observed. The first dose release was

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established in pH 1.2 for a period of 2 h, followed by pH 6.8. The second dose pellets were

passed through pH 1.2, pH 6.8 followed by pH 7.5 for the rest of the study. The authors

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concluded that multiparticulate dosage form of ketoprofen was able to relieve circadian
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symptoms of rheumatoid arthritis during midnight and early morning. Maniruzzaman et al [27]

prepared extrudes of cationic model drug propranolol HCl by extrusion and spheronization
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technique with the anionic polymers Eudragit L100 and Eudragit L100-55. Taste masking was
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determined by using e tongues. Intermolecular interactions as the mechanism of successful taste

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masking was ascertained from FT-IR spectroscopy and NMR studies. Aguilar et al [28] used

polyurethane and Eudragit® L100-55 as nanofiber by belectrospinning technique. The composite

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mat has adequate mechanical properties and in vitro cell biocompatibility indicating that the

material can be used for drug eluting stent cover application. De Barros et al [29] designed a
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laminated polymer film formulation for enteric delivery of live vaccine and probiotic bacteria.
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Eudragit L 100-55 based polymeric laminate successfully protected dried probiotic or vaccine

live bacterial cells from SGF for 2 h, and subsequently released all viable cells within 60 min of

transfer into simulated intestinal fluid.

Eudragit S (S-100, 12,5 and FS 30 D)

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Eudragit S 100 and S 12,5 are anionic copolymers based on methacrylic acid and methyl

methacrylate. Eudragit S100 is solid substance in the form of white powder with a faint

characteristic odour. Eudragit S12,5 is a colourless and clear to slightly cloudy liquid with

characteristic odour of isopropyl alcohol. Both grades have molecular weight, acid value and

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glass transition temperature approximately 125,000 g/mol, 190 mg KOH/g polymer and > 1500 C

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respectively. Eudragit S 100 is available in the form of powder. Eudragit S 12,5 is available in

the form of organic solution (12.5 %). Both grades dissolve at pH 7.0 and used for colon targeted

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drug delivery.

Eudragit FS 30D is a milky white liquid of low viscosity with a faint characteristic odor.

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It is the aqueous dispersion of an anionic copolymer based on methyl acrylate,
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methylmethacrylate and methacrylic acid. It is insoluble in acidic media, but dissolves by salt

formation above pH 7.0. Apart from its enteric properties, its dissolution at a higher pH value
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allows targeted colon drug delivery. Its molecular weight, acid value and glass transition
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temperature are approximately 2,80,000 g/mol, 70 mg KOH/g polymer and 480C respectively.
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Due to low minimum film forming temperature only small amounts of plasticizer are required to

get a smooth film formation. It is available in the form of aqueous dispersion (30%).
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A current review on recent research publications based on Eudragit S 100 is described as

follows. It is used in formulation of transdermal patch, nanoparticles, microparticles,

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microballons, solid dispersions and spherical crystals. It has been used for various applications
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such as colon specific drug delivery, sustain release, bioavailability enhancement, improvement

in micromeritic properties etc as shown in Table 5. Madan et al [40] evaluated the sustain release

potential of Eudragit S100 by formulating transdermal patches of donepezil using various

polymers along with plasticizer and penetration enhancer. Eudragit S100, Eudragit E100 and
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HPMC were used as matrix forming agents in the formulation of patches. They concluded that

transdermal patch can extend the release of donepezil for many hours with enhanced

bioavailability. Hence Eudragit S 100 can be used to extend release of domepezil in transdermal

patches. Li et al [16] evaluated colon specific drug delivery potential of Eudragit S 100 based

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enteric coating of model drug. Enteric coating was achieved by applying Eudragit S 100 to

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microencapsulated 5-Flurouracil and leucovorin coloaded with folate-chitosan nanoparticles.

When the pH value reached the soluble threshold of Eudragit S-100, a constant and slow drug

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release was observed. Eudragit S100 can be used for selectively targeting drugs to colon in the

chemotherapy of colon cancer. Nandy et al [41] formulated and characterized delayed release

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multi particulates system of indomethacin. Microspheres were formulated by using a novel quasi
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emulsion solvent diffusion technique using combination of ethyl cellulose (EC) and Eudragit RS

100/Eudragit S100;. Drug release decreased significantly (p<0.05) with increase in amount of
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Eudragit polymer. Therefore this approach suggested that the combination of EC and Eudragit
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S100 microspheres may be useful for the delivery of maximum amount of indomethacin to the
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colon.

No literature was found for Eudragit S 12,5 in pubmed indexed journals. But few articles
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were published on the use of Eudragit FS 30 D in various dosage forms such as multiparticles,

tablets and capsules for enteric coating as shown in Table 5. Dreu et al [42] produced multiple-
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unit tablet compressed from enteric-coated pellets. An optimal coating was obtained by mixing
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two acrylic polymers: relatively brittle Eudragit® L30 D-55 with more flexible Eudragit® FS 30

D. The final formulation released 9 % drug in acidic medium. In addition to coating, biconvex

shape of tablet and protective coating of Kollidon VA 64 also played a significant role in

achieving enteric coating. Huyghebaert et al [43] developed an alternative method for enteric
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coating of HPMC capsules that avoids the sealing step before coating, resulting in ready-to-use

enteric-coated capsules for the use in retail or hospital pharmacy or R&D sections of

pharmaceutical industry and for the production of enteric-coated heat and moisture sensitive

biomaterials. The release of thymidine in 0.1N HCl after 2 h from capsules coated with Eudragit

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L30D-55, Eudragit FS 30 D, Aqoat AS-HF and Sureteric was 0.6+/-.03, 0.6+/-0.3, 1.2+/-0.2 and

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7.3+/-1.9% respectively. The alternative method was reproducible and offered a way to

overcome the time-consuming and expensive sealing step required using the conventional

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coating procedure.

Eudragit NE 30D, NE 40D and NM 30D

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Eudragit NE 30D, NE 40D and NM 30 D are the aqueous dispersion of a neutral
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copolymer based on ethyl acrylate and methyl methacrylate. These are milky white liquid of low

viscosity with a faint characteristic odour. All the three grades have minimum film forming
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temperature of 50 C. Both NE 30D and 40 D are having a molecular weight of approximately

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7,50,000 g/mol whereas NM30 D have molecular weight of 6,00,000 g/mol. Glass transition
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temperature (Tg) of NE 30 D and 40D are ~80 C whereas NM 30 D is having glass transition

temperature of ~11 0C. Eudragit NE 30D, NE 40 D and NM 30 D are available in the form of
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aqueous dispersion 30, 40 and 30 % respectively. All are highly flexible in nature and does not

require incorporation of plasticizer. They are used in formulation of controlled release products
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which are independent of pH of gastrointestinal tract.

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An extensive review on Eudragit NE 30D revealed that it is used for modified release

formulations in various dosage forms such as multiparticles, microparticles, pellets, films etc as

shown in Table 6. Amrutkar et al [52] designed multiparticulate floating drug delivery system of

zolpidem tartarate to prolong the gastric residence time and to improve bioavailability. The
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system consists of effervescent layer (sodium bicarbonate) and polymeric layer (Eudragit NE

30D) membrane. In-vitro drug release of the system were dependent on Coating level of the

polymeric membrane (Eudragit(®) NE 30D) played a significant role in drug release. Kumaria et

al [53] developed and evaluated Loratidine buccal films for allergic rhinitis. Polymeric

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buccoadhesive films of loratidine were prepared using hydroxypropylmethyl cellulose (HPMC)-

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E5 and K100 blend and Eudragit® NE 30D as retardant. Films were prepared using solvent-

casting method. Increase in Eudragit® NE 30 D content in the film decreased the hydration,

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erosion and drug release, but enhanced the mucoadhesion time.

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Current literature review on Eudragit NE 40 D suggests that it is used for various
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pharmaceutical applications like modified release, enhancement of bioavailability etc as

bucoadhesive films and non occlusive dermal therapeutic systems as shown in Table 6. Kumria
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et al [54] prepared buccoadhesive films of prednisolone by solvent-casting method using

hydroxyl propyl methyl cellulose (K100), Carbopol 940 and/or Eudragit® NE 40 D. Buccal
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route was found as a viable option for delivery of prednisolone. Minghetti et al [55] prepared
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self-adhesive matrix made of a mixture of Plastoid E 35 L, an adhesive hydrophilic polymer, and

eudragit NE 40 D, a nonadhesive hydrophobic polymer able to modify the drug release. All
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systems sustained drug release for at least 24 h. No literature was found for Eudragit NM 30D
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based formulations in pubmed indexed journals.

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Eudragit RL 30 D, RLPO, RL100 and RL 12,5

Eudragit RL 30 D, RLPO, RL100 and RL 12,5 are copolymers of ethyl acrylate, methyl

methacrylate and a low content of methacrylic acid ester with quaternary ammonium groups. The

ammonium groups are present as salts and make the polymers permeable. RL 30D is a milky

white liquid of low viscosity with a faint characteristic odour. Molecular weight of RL 30D is
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approximately 32,000 g/mol. Its minimum film forming temperature and glass transition

temperature are 400C and 550C respectively. Alkali value of RL 30D is 32.3 mg KOH per g of

polymer. RL 30D is available in the form of 30% aqueous dispersion. RL 30D exhibit pH

dependent swelling. RL 30D is primarily used in the formulation of sustained release products.

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Eudragit RLPO is a solid substance available in the form of white powder with a faint amine like

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odour whereas eudragit RL100 is a solid substance available in the form of colourless, clear to

cloudy granules with a faint amine like odour. Molecular weight, alkali value and glass transition

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temperature of both RLPO and RL 100 are same i.e. 32,000 g/mol, 28.1 mg KOH/g polymer and

700C respectively. RLPO and RL100 is mainly used for customized release profile by

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combination of RL and RS grades in different ratios and they are also suitable for matrix
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structures. Eudragit RL 12,5 is light yellow liquid of low viscosity, clear to slightly cloudy with a

characteristic odour of solvents. RL 12,5 is available in the form of a 12.5% organic solution. Its
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molecular weight, alkali value and applications are same as RLPO.

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An extensive literature review on Eudragit RL 30D revealed that this polymer is

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primarily used for controlled release DDS as shown in Table 7. Kibria et al [60] investigated the

effect of physico-chemical properties of the polymers vis-à-vis eudragit RL30D and RS30D on
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the release profile of ketoprofen from pellets. Extruded and spheronized pellets were coated with

15% (w/w) polymers Eudragit RL 30 D and Eudragit RS 30 D. It was revealed that Eudragit RL
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30 D has the effect to increase the initial drug release more significantly than RS 30D. Lingam et
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al [61] formulated matrix type multiple-unit (minitablets) floating drug delivery system for

captopril. The system consists of core units which are coated with three successive layers vis-à-

vis inner seal coat, effervescent layer and an outer gas-entrapped polymeric membrane of an

polymethacrylates. Eudragit RL30D and its combination formulations exhibited floating.

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Review on Eudragit RLPO is primarily used for sustaining drug release in diverse drug

delivery systems like nanoparticles, mucoadhesive tablets and patches, solid dispersions etc as

shown in Table 7. Singh et al [62] investigated the effect of iron oxide in the development of

mucoadhesive tablets of cinnarizine using Eudragit RLPO. Eudragit RLPO and iron oxide

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exhibited potential for gastroretentive and mucoadhesive drug delivery systems. Pandey et al

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[63] attempted site specific drug delivery by formulating bilayered gastroretentable

mucoadhesive patch (stomach). Both Eudragit RSPO and RLPO were used for formulation of

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patch. Patches could control the drug release up to 12 h, with mucoadhesion. Sahoo et al [64]

formulated solid dispersion of verapamil using Eudragit RLPO or Kollidon SR to sustain drug

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release. Extended the drug release upto 12 h was attained in case of Eudragit RLPO.
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A widespread literature review on Eudragit RL 100 revealed that it is used for controlled

release and bioavailability improvement approaches in various dosage forms such as

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nanoparticles, tablets, buccal films, transdermal patches, ophthalmic inserts etc as shown in
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Table 7. Singh et al [65] prepared atazanavir nanoparticles loaded with Eudragit RL 100 to
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improve oral bioavailability. These nanoparticles were prepared by nanoprecipitation method.

Eudragit L100 based nanoparticles showed improved bioavailability potential. Ofokansi et al

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[66] prepared ibuprofen tablets from interpolyelectrolyte complexes (IPECs), formed between

Eudragit RL100 and chitosan, by nonstoichiometric method, and tablets based on the above
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complex by wet granulation method. The complex was capable of preventing drug release in the
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stomach and small intestine and helped colon specific drug delivery. Palem et al [67] prepared

domperidone (DOM) hot-melt extruded (HME) buccal films by using combination of HPMC E5

LV or Eudragit RL100 as polymeric carriers along with some other carriers exhibited 1.5 times

improved bioavailability. Thakur et al [68] formulated the bioerodable insert of azithromycin to

 ACCEPTED MANUSCRIPT

prolong the release time and improve the ocular availability. Azithromycin insert was prepared

using hydroxyl propyl methyl cellulose (HPMC) and Eudragit RL100. The formulation

(comprising of 1.5% HPMC and 3% Eudragit RL100) showed release of drug over a 12 h in a

steady and controlled manner. No research articles found for Eudragit RL 12,5 in pubmed

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indexed journals.

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Eudragit RS 30D, RSPO, RS 100 and RS 12,5

Eudragit RS 30D, RSPO, RS100 and RS 12,5 is a copolymer of ethyl acrylate, methyl

SC
methacrylate and a low content of methacrylic acid ester with quaternary ammonium groups. The

ammonium groups are present as salts. Presence of salts makes them more permeable. Eudragit

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RS 30 D is a liquid of low viscosity with milky white color showing faint characteristic odour.
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Eudragit RSPO is white powder with a faint amine like odour. Eudragits RS 100 is colorless

granule with a faint amine like odour. Eudragit RS 12,5 is a light yellow liquid of low viscosity,
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clear to slightly cloudy with a characteristic odour of the solvents. Molecular weight of each of
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the above grades is 32,000 g/mol. Eudragit RS 30D, RSPO, RS100 and RS 12,5 are available in
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the form of 30% aqueous dispersion, powder, granules and 12.5 % organic solution respectively.

All the above four grades of Eudragit are insoluble. They exhibit low permeability with pH
EP

independent swelling. These polymers are used for controlled and customized release profile by

combination of RL and RS grades in different ratios.

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Eudragit RS 30 D is extensively used for formulation of sustain release products. The

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current literature survey suggests that this polymer has been used in formulation of pellets,

coating of pellets osmotically driven pellets etc as shown in Table 8. Piao et al [82] developed

sustained release osmotic pellet coated of oxymatrine. Extrusion/spheronization followed by

coating with Eudragit RS 30 D was adopted. They found that the F3 formulation, prepared with
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20% NaCl and an 8% coating level (Eudragit RS 30 D), showed a continuous NaCl-induced

water influx into the pellets providing a gradual sustained release of OMT for over 12 h. Kibria

et al [60] investigated the release of ketoprofen from pellets to study the effect of physico-

chemical properties of polymers. The drug containing core pellets were prepared by extrusion

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spheronisation technique and subsequently coated with 15% (w/w) polymer load of the

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combination of Eudragit RL 30 D & Eudragit RS 30 D. It was revealed that Eudragit RL 30 D

has the effect to increase the initial drug release more significantly where as Eudragit RS 30 D

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has the effect to minimize the initial drug release but increase the terminal drug release more

significantly.

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An extensive review on research publication on Eudragit RSPO revealed that it is mainly
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used in the sustaining drug release as shown in Table 8. Eudragit RSPO has been used in the

formulation of microballons, tablets, microspheres and microtablets. Porwal et al [83] prepared

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microballons of propranolol HCl by the non-aqueous oil in oil emulsion solvent diffusion
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evaporation method using Eudragit RSPO as polymer. The drug release from microballoons
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showed a biphasic pattern with an initial burst release, followed by sustained release for 12 h.

Abbaspour et al [84] prepared and characterized ibuprofen pellets based on Eudragit RSPO and
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RLPO or their combination. Eudragit RLPO compare with Eudragit RSPO resulted in pellets

with high crushing strength; however, Eudragit type did not have a significant effect on elastic
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modulus.
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Literature review on applications of eudragit RS100 suggests that it has been used

extensively in the formulation of following types of dosage form vis-à-vis nanoparticle, bilayer

tablet, matrix tablet, transdermal patch, vaginal tablets etc as shown in Table 8. Zhang et al [85]

formulated nanostructured lipid carrier (NLC) surface modified with Eudragit RS100 Model
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drug genistein was selected. NLC was produced using the melt-emulsification technique

followed by surface absorption of Eudragit RS 100. The Eudragit RS 100 increased the surface

zeta potential from -7.46 mV to +13.60 mV, by uniformly forming a spherical coating outside

the NLC surface, as shown by transmission electron microscopy images. Particle size growth

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was inhibited by Eudragit RS 100. Increased corneal penetration producing a 3.3-fold increase in

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apparent permeability coefficients was attributed to Eudragit RS100. Baviskar et al [86] prepared

matrix-type transdermal drug delivery system of lornoxicam with the addition of hydrophilic and

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hydrophobic polymers in different ratios. Transdermal patches of lornoxicam were designed with

ethyl cellulose:polyvinylpyrrolidone and Eudragit RL 100:Eudragit RS 100 in different ratios

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with propylene glycol as plasticizer (5%) and tween 80 as permeation enhancer using the solvent
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evaporation technique. It was observed that both the patches significantly controlled

inflammation and showed analgesic effect from the first hour (P < 0.05). Formulations A3 and
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B3 were found to enhance the bioavailability of lornoxicam by 3.1 and 2.7 times, respectively,
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compared to the oral dosage form. Hence, lornoxicam can be formulated into transdermal
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patches for sustain release characteristics. As far as Eudragit RS 12,5 is considered no such

research article is published in any indexed research journals.

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RECENT PATENTS ON EUDRAGIT BASED FORMULATIONS

Recent reviews on various patents published on Eudragit based formulation were

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collected. It was observed that Eudragit based formulation has been patented for diversified
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applications. They are used for colonic drug delivery, bitter taste masking, improved hardness,

enhanced stability, improved bioavailability, prolonged drug release etc as shown in Table 9.

Antoine et al [97] prepared pectin beads cross linked with zinc or any divalent cation for colonic

delivery of drugs. The beads were then coated with Eudragit- FS 30D, LE 30D and NE 30D. The
 ACCEPTED MANUSCRIPT

use of zinc cations to crosslink the pectin is particularly preferred to provide a stable metallo-

enzyme formulation for the lower intestinal or colonic delivery of such an enzyme. Choy et al

[98] patented hybrid of ursodeoxycholic acid-synthetic hydrotalcite-and Eudragit for bitter-taste-

masking and improved body absorption rate with high solubility. Ursodeoxycholic acid is bitter

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in taste. The inventors found that a hybrid obtained by incorporating ursodeoxycholic acid

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between the layers of hydrotalcite, which is used as an antacid and a stomachic, and then coating

with Eudragit, which is an enteric coating, blocks the bitter taste of ursodeoxycholic acid and

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simultaneously shows improvement of dissolution rate and high bioavailability. Shojaei et al [99]

patented on how the Eudragit L100-55 played a significant role in achieving desired hardness for

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tablets. The present invention relates to a pharmaceutical composition comprising a
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pharmaceutically active agent and a Eudragit L 100-55 which is useful to achieve the required

release and desired compressibility. Tummala et al [100] patented enhancement of bioavailability

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of the curcumin by complexing curcuminoid with Eudragit®. Chen et al [101] prepared stable
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and sustain release solid dispersions of misoprostol with various grades of Eudragit RS
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series, Eudragit RL series, Eudragit S and Eudragit L. Periano [102] patented stable formulation

of sennoside by granulation of senna extract (20% sennosides) with Eudragit L100 and then
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coated with Eudragit L 30 D 55. This product was stable for a long time and has good

organoleptic properties (taste and odor). Christophe et al [103] patented microgranules of

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ketoprofen using eudragit RL and RS for prolonged release. Aqueous dispersions of Eudragit RL
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and RS were used for the preparation of microgranules. Robert et al [104] attempted to stabilize

benzimidazole derivative proton pump inhibitors. The present invention provides a composition

containing a benzimidazole derivative proton pump inhibitor and a polymeric base selected from

the group consisting of cholestyramine-OH, Eudragit E-PO, chitosan, or a mixture thereof. The
 ACCEPTED MANUSCRIPT

composition of the present innovation provides improved stability for the benzimidazole

derivative proton pump inhibitor under naturally occurring humidity ranges so that degradation

during storage and in the stomach is minimized. It can be easily manufactured by directly

admixing the benzimidazole derivative proton pump inhibitor with the polymeric base.

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CONCLUSION

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This represents a comprehensive review of 107 references where various grades of

Eudragit were used to develop formulations with widespread applications. The various drugs and

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techniques used in Eudragit based formulations have been described in sufficient detail to give

the reader a basic understanding about the role of Eudragit in different formulations. Hence this

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review manuscript can be used as ready reckoner for researchers to develop Eudragit based drug
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delivery systems.

ACKNOWLEDGEMENTS
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The authors are thankful to management and principal, Roland Institute of Pharmaceutical
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sciences, Berhampur, India for support and encouragement.

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soluble drug used to treat stress ulcers (I): in vitro and in vivo evaluation in rabbits. Drug

Dev Ind Pharm. 2013; 39:1230-1237.

EP

83. Porwal A, Swami G, Saraf S. Preparation and evaluation of sustained release

microballoons of propranolol. Daru. 2011; 19 :193-201.

C

84. Abbaspour MR, Sadeghi F, Garekani HA. Preparation and characterization of ibuprofen
AC

pellets based on Eudragit RS PO and RL PO or their combination. Int J Pharm. 2005;

303:88-94.
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85. Zhang W, Li X, Ye T, Chen F,Yu S, Chen J, Yang X, Yang N, Zhang J, Liu J, Pan

W, Kong J. Nanostructured lipid carrier surface modified with Eudragit RS 100 and its

potential ophthalmic functions. Int J Nanomedicine. 2014; 9:4305-4315.

86. Baviskar DT, Parik VB, Jain DJ. Development of matrix-type transdermal delivery of

PT
lornoxicam: in vitro evaluation and pharmacodynamic and pharmacokinetic studies in

RI
albino rats. PDA J Pharm Sci Technol. 2013; 67:9-22.

87. Kibria G, Islam KM, Jalil RU. Stability study of ambroxol hydrochloride sustained

SC
release pellets coated with acrylic polymer. Pak J Pharm Sci. 2009; 22:36-43.

88. Krejcová K, Rabisková M, Vetchý D, Tomásek V, Prokopová A. The effect of

U
polymeric dispersion type on the release of diclofenac sodium from coated pellets. Ceska
AN
Slov Farm. 2007; 56:190-199.

89. Roni MA, Kibria G, Jalil RF. Formulation and in vitro Evaluation of Alfuzosin Extended
M

Release Tablets Using Directly Compressible Eudragit. Indian J Pharm Sci. 2009;
D

71:252-258.
TE

90. Sahoo SK, Dhal S, Mohapatro P, Behera BC, Barik BB. Effect of processing temperature

on Eudragit RS PO microsphere characteristics in the solvent evaporation process.

EP

Pharmazie. 2007; 62:638-639.

91. Boza A, Caraballo I, Alvarez JF, Rabasco AM, Evaluation of Eudragit RS-PO and
C

Ethocel 100 matrices for the controlled release of lobenzarit disodium. Drug Dev Ind
AC

Pharm. 1999; 25:229-233.

92. Rey H, Wagner KG, Wehrlé P, Schmidt PC. Development of matrix-based theophylline

sustained-release microtablets. Drug Dev Ind Pharm. 2000; 26:21-26.

 ACCEPTED MANUSCRIPT

93. Tiwari R, Gupta A, Joshi M, Tiwari G. Bilayer Tablet Formulation of Metformin HCl

and Acarbose: A Novel Approach To Control Diabetes. PDA J Pharm Sci Technol. 2014;

68:138-152.

94. Mathur V, Nagpal K, Singh SK, Mishra DN. Comparative release profile of sustained

PT
release matrix tablets of verapamil HCl. Int J Pharm Investig. 2013; 3:60-65.

RI
95. Tayel SA, El-NabarawiMA, Tadros MI, Abd-Elsalam WH. Positively charged polymeric

nanoparticle reservoirs of terbinafine hydrochloride: preclinical implications for

SC
controlled drug delivery in the aqueous humor of rabbits. AAPS PharmSciTech. 2013; 14

:782-793.

U
96. Gupta NV, Natasha S, Getyala A, Bhat RS. Bioadhesive vaginal tablets containing spray
AN
dried microspheres loaded with clotrimazole for treatment of vaginal candidiasis. Acta

Pharm. 2013; 63:359-372.

M

97. AntoineA, HélèneH. Colonic delivery using zn/pectin beads with a eudragit coating. US
D

Patent: 20080124279. 2008; May 29.

TE

98. ChoyJ. H, ChoiG. E, ParkM. C, et al.Ursodeoxycholic acid-synthetic hydrotalcite-

eudragit hybrid, pharmaceutical composition containing the same and method for
EP

preparing the same.US Patent: 20120156263. 2012; Jun 21.

99. Shojaei AH, Melissa EC. Modified release tablet formulations with enhanced mechanical
C

properties. US Patent: 20070104782. 2007; February 08.

AC

100. Tummala H, Kumar S. Curcuminoid complexes with enhanced stability, solubility and/or

bioavailability.US Patent: 20140271530. 2014; September 18.

101. David C, Rong-jen T, Hue-in L. Improved stabilization of misoprostol. European Patent

:0896823. 2002; September 25.

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102. JorgeP. H. Coated senna extract granules. WO/2011/014976. 2011; October 02.

103. Lebon C, Marechal D, Suplie P. ketoprofen microgranules, method for preparing same

and pharmaceutical compositions. WO/2000/064432. 2000; November 11.

104. Robert F, Narayan R, Joseph Z et al., Formulation stabilizer for proton pump

PT
inhibitors.US Patent :20060013880. 2006; January 19.

RI
105. Stevens H, Chariot M, Arnold F. Sustained release pharmaceutical composition.

EP0322277. 1992; January 22.

SC
106. Andremont A, Huguet H. Colonic delivery of metallo-dependent enzymes. US Patent:

20080199528. 2008; August 21.

U
107. Isa O. Oral drug delivery formulations. US Patent: 20150250733. 2015; September 10.
AN
M
D
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C EP
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Table 1, Tabulation for solubility of various grades of Eudragit [1]

Grades of Eudragit Recommended solvents Solubility/Permeability

Eudragit E12,5, Acetone, alcohol Soluble in gastric fluid to pH 5
Eudragit E100,

PT
Eudragit EPO
Eudragit L 100-55, Acetone, alcohol for L100-55 Soluble in intestinal fluid from pH

RI
Eudragit L 30 D-55, Water 5.5
Eastacryl 30D,

SC
Kollicoat 30D
Kollicoat 30DP
Acryl EZE
Acryl EZE MP
U
AN
Eudragit L-12.5P, Acetone, alcohol Soluble in intestinal fluid from pH
Eudragit L-12.5, 6
M

Eudragit L 100
Eudragit S 12.5P, Acetone, alcohol Soluble in intestinal fluid from pH
D

Eudragit S 12.5, 7
Eudragit S 100
TE

Eudragit FS 30D Water

Eudragit RL12.5, Acetone, alcohol High permeability
EP

Eudragit RL100,
Eudragit RD 100
Eudragit RL PO
C

Eudragit RL 30D Water

AC

Eudragit RS 12.5 Acetone, alcohol Low permeability

Eudragit RS 100
Eudragit RS PO
Eudragit RS 30D Water
Eudragit NE 30D, Water Swellable, permeable
Eudragit NE 40D
 ACCEPTED MANUSCRIPT

Table 2, Reported literature on Eudragit E 100, E 12,5 and EPO

Drug name Dosage form/ Method of Applications Refer

delivery Preparation ences
system
Eudragit E 100
Flurbiprofen Opthalmic Ionic Constant rate of delivery [2]

PT
aqueous complexation and improved
solution permeation
Clotrimazole Transdermal Eutectic mixture Improved drug transport [3]

RI
spray across the skin
Triclosan Nanoparticles Emulsification- Improved drug delivery [4]
diffusion by

SC
solvent
displacement
method
Tramadol Orally Mass extrusion Bitter taste masking [5]

U
Hydrochloride disintegrating technique
tablet
AN
Carvidilol Nanoparticles Nanoprecipitation Improved therapeutic [10]
efficacy (Faster
dissolution)
M

Ranitidine Floating Solvent Improved absorption [11]

hydrochloride microspheres evaporation and bioavailability
method
D

Eudragit E 12,5
* * * * *
TE

Eudragit EPO
Clindamycin Oral Drug coated to Improved pediatric and [6]
HCl disintegrating MCC beads geriatric patient
tablet followed by compliance by taste
EP

coating of eudragit masking.

EPO suspension
followed by
compression
C

Osthole Solid Hot-melt extrusion Improved dissolution [12]

dispersion rate and bioavailability
AC

Atorvastatin Amorphous Direct compression Improved [7]

solid bioavailability by
dispersions increasing its gastric
compressed to solubility in a stable oral
orally disintegration tablet
disintegrating
tablet
Bifendate solid Hot-melt extrusion Enhanced [13]
dispersions bioavailability
 ACCEPTED MANUSCRIPT

Meloxicam Nanoparticles Nanoprecipitation Improved anti- [8]

method inflammatory activity
compared to suspension.
Andrographolide pH sensitive Nanoprecipitation Improved the oral [14]
nanoparticle technique bioavailability with
suspension shorter Tmax
Aciclovir and liposomes High-pressure Cationic polymers had a [9]

PT
Minoxidil homogenization stabilising effect
Diclofenac Polycomplex Interpolyelectrolyte Considerable pH- [15]
sodium and matrices complexes (IPEC) sensitive swelling in

RI
Theophylline between acidic and neutral media
countercharged
polymers

SC
*
No literature found

U
AN
M
D
TE
C EP
AC
 ACCEPTED MANUSCRIPT

Table 3, Reported literature on Eudragit L 100 and 12,5

Drug name Dosage form/ Method of Application Refere

delivery system Preparation nce
Oral insulin Combination of Self In-situ Enhancing the oral [16]
nanoemulsifying emulsification absorption and efficacy of
DDS & enteric insulin and eudragit L 100

PT
coated capsules as a enteric polymer.
Curcumin Microsponge for Quasi emulsion Eudragit L 100 prevented [17]
colon targeting solvent the premature release of

RI
diffusion curcumin in upper GIT.
method
Lacidipine Lyophilised Thin film Lipotomes enhanced oral [20]

SC
Lipotomes filled hydration bioavailability and
into enteric coated technique Eudragit L 100 as a
capsules. enteric polymer.
Dipyridamole floating alginate Ionic cross Prolonged stomach [21]

U
beads combined linking and retention time due to
with the solid solid dispersion CaCO3 and modified drug
AN
dispersion technique release due to Eudragit
L100 and RLPO.
Alendronate Enteric-coated Nanotechnology Resist the release of ALS [18]
M

sodium nanoliposomes in acidic environments

(ALS) and enhanced the
bioavailability
Pantoprazole Delayed release Wet granulation Sustained release in [19]
D

tablets method intestine and significant

followed by reduction in ulcer
TE

enteric coating formation

Insulin Thiolated eudragit Nanotechnology Facilitate insulin [22]
based nanoparticles permeation through the
EP

with reduced intestinal epithelium.

glutathione.
Eudragit L 12,5
* * * * *
C

*
No literature found
AC
 ACCEPTED MANUSCRIPT

Table 4, Reported literature on Eudragit L30 D-55 and L 100-55

Drug name Dosage form/ Method Application Refer

delivery ences
system
Eudragit L 30D-55
Oral Chlorea Microparticles Spray dried An approach to a cold chain [30]

PT
vaccine technique free and effective oral
cholera vaccine.
Tenoxicam Transdermal Casting Sustain drug release [24]

RI
self-adhesive evaporation
films technique
Esomeprazole Enteric coated Coating Better dissolution & stable [23]

SC
magnesium tablet for a period of 3 months.
trihydrate
Tamsulosin Controlled- Extrusion/sphero Controlled release [31]
hydrochloride release capsule nization method
Ranitidine leaky enteric-
U
Extrusion- Maintain or increase the [25]
AN
hydrochloride coated pellets spheronization bioavailability of drugs that
followed by have a window of
spray coating absorption
Diclofenac Enteric coated Fluidized-bed The mixture of Eudragit [32]
M

sodium pellets coating NE30D and Eudragit L30D-

compressed 55 could be used to prepare
into tablets enteric pellets.
D

Mycoplasma Microsphere Co spray drying Oral microspheres vaccine [33]

hyopneumoniae prepared by a co-spray
TE

oral vaccine drying method can provide

effective protection against
M M. hyopneumoniae
infection in pigs.
EP

Eudargit L 100-55
Ketoprofen pH-responsive Extrusion- To relieve circadian [26]
dual pulse spheronization symptoms of rheumatoid
C

multiparticulat & Fluid bed arthritis during midnight

e dosage form coating. and early morning
AC

Propranolol HCl Taste mask Hot melt Drug polymer [27]

formulation extrusion (Single intermolecular interactions
screw) as the mechanism of
successful taste masking.
Amifostine Enteric Spray drying Oral administration of [34]
microcapsules technique amifostine microcapsules
provided effective
radioprotection compared to
 ACCEPTED MANUSCRIPT

the bulk drug.

Omeprazole Nanoparticles Ultrasonic Nanoparticles showed a [35]
dispersion and strong pH-sensitive release
diffusion in vitro.
solidification
Gemcitabine Enteric Double emulsion Oral absorption could be [36]

PT
Microparticles method increased with
mucoadhesive polymer
Domperidone Oral Direct Fast and pH-dependent [37]
disintegrating compression release

RI
tablet method
Paclitaxel Nanofiber Electrospinning pH dependent release of [28]
process paclitaxel on duodenal stent

SC
composite mat
cover application.
Live bacterial Polymer film Film casting Eudragit alone successfully [29]
cells as laminate protected dried probiotic or

U
attenuated vaccine LBC from SGF for
vaccines 2 h, and subsequently
AN
released all viable cells
within 60 min of transfer
into SIF.
Cinnarizine Microparticles Coacervation pH responsive drug release [38]
M

technique
Insulin Enteric Complex Complex coacervation [39]
nanoparticles coacervation process using chitosan
D

method and Eudragit L100-

55 polymers may provide a
TE

useful approach for

entrapment of hydrophilic
polypeptides without
affecting their
EP

conformation.
C
AC
 ACCEPTED MANUSCRIPT

Table 5, Reported literature on Eudragit S 100, 12,5 and FS 30 D

Drug name Dosage form/ Method of Application Refere

delivery system Preparation nces
Eudragit S 100
Donepezil Transdermal Solvent casting Extended release, [40]
Patches technique enhanced bioavailability,

PT
avoids the first pass effect
5-fluourouacil (5- Nanoparticles Ionic gelation Selectively targeting [16]
FU) and leucovorin microencapsulat followed by drugs to colon in the

RI
ed with enteric solvent chemotherapy of colon
polymers evaporation cancer.
method

SC
Raloxifene Nanocapsules Interfacial Best activity was [44]
hydrochloride deposition of observed for RH-loaded
preformed Eudragit S100
polymer nanocapsules after 72 h

U
Indomethacin Multi- Novel quasi Combination of EC and [41]
particulates emulsion Eudragit S100 delivered
AN
system in the solvent maximum amount of drug
form of diffusion to colon.
microspheres technique
M

Dextromethorphan Solid dispersion Solvent Solid dispersion of drug- [45]

(modified in situ evaporation Eudragit S 100 to
gelling alginate method overcome the problems of
formulations). dose dumping after the
D

rupture of the pH
dependent alginate gels.
TE

Nizatidine Encapsulated Emulsion Sustain release and [46]

microballoons solvent increased residence time
diffusion
EP

method
5-Flurouracil Enteric coated Dextran Eudragit S100 retard the [47]
dextran Microspheres release of drug in gastric
microspheres by and intestinal pH and the
C

emulsification- drug released in colon due

crosslinking to the degradation of
AC

method and dextran by colonic

enteric coating enzymes.
by oil-in-oil
solvent
evaporation
method.
Peptide Val-Leu- Enteric coated Double Nanoparticles almost [48]
Pro-Val-Pro-Arg nanoparticles emulsion completely released at pH
(VLPVPR) method 7.4 after 8 h reduced
 ACCEPTED MANUSCRIPT

followed by blood pressure for more

freeze drying than 30 h
Flurbiprofen Microspheres Oil/oil Colon specific drug [49]
emulsification delivery
method
Mebendazole Spherical Solvent change Spherical crystals with [50]
crystals method improved micromeritic

PT
properties.
Eudragit S 12,5
* * * * *

RI
Eudragit FS 30 D
Theophyline Multiparticulate Direct Delayed release property [51]
(enteric coated compression was preserved.

SC
with FS 30 D)
compressed in to
tablets
Tartrazine (model Multiple-unit Film coating An optimal coating was [42]

U
substance) tablet technique obtained by mixing two
compressed from acrylic polymers:
AN
enteric-coated relatively brittle
pellets Eudragit® L30 D-55 with
more flexible Eudragit®
M

FS 30 D.
Thymidine Enteric-coated Optimised Ready-to-use enteric- [43]
HPMC capsules coating process( coated HPMC capsules
D

fluid bed for the use in retail or

apparatus) hospital pharmacy or
TE

R&D sections of
pharmaceutical industry.
*
No literature found
C EP
AC
 ACCEPTED MANUSCRIPT

Table 6, Reported literature on Eudragit NE 30 D

Drug name Dosage form/ Method of Application Refer

delivery system Preparation ences
Eudragit NE 30 D
Zolpidem Multiparticulate Coated with Rapid floating and modified [52]
tartarate floating drug effervescent drug release was obtained.

PT
delivery system layer and
(pellets) polymeric
membrane

RI
Loratidine Prolonged Solvent-casting Mucoadhesion and release [53]
release method retardation was achieved
Buccoadhesive with HPMC and eudragit

SC
film NE 30 D respectively.
Theophylline or Multiparticulate Extrusion- Modified release [56]
cimetidine DDS spheronization
followed by

U
coating.
Venlafaxine Pellets Extrusion/ Differences in the film [57]
AN
hydrochloride spheronization micro-structure and surface
followed by roughness influence the in
coating vivo release
M

Tamsulosin Sustain Release Single-step Optimum ratio of [58]

hydrochloride microparticles matrix coating Aquacoat® and Eudragit®
NE30D in the matrix (9:1)
provides a sustained-release
D

Urapidil Drug layer Centrifugal Improvement in [59]

pellets followed granulation and bioavailability
TE

by coating fluid bed coating

Eudragit NE 40 D
Prednisolone Buccoadhesive solvent-casting Enhanced bioavailability [54]
EP

films method
Miconazole Nonocclusive Matrix system In vitro control of drug [55]
nitrate dermal release for at least 24 h
therapeutic
C

system
Eudragit NM 30 D
AC

* * * * *
*
No literature found
 ACCEPTED MANUSCRIPT

Table 7, Reported literature on Eudragit RL 30 D, RLPO, RL100 and RL 12,5

Drug name Dosage form/ Method of Application Refere

delivery system Preparation nces
Eudragit RL 30D
Diltiazem HCl Matrix Tablets Dry mixing and Controlled release [69]

PT
direct
compression
followed by

RI
coating with
Eudragit NE 30D
Ambroxol Pellets Extrusion- Stability was dependent on [70]

SC
hydrochloride spheronization storage condition and
technology physicochemical property
followed by of the polymer.
coating with

U
Eudragit NE 30D
Ketoprofen Pellet Extrusion Proper selection of [60]
AN
spheronisation polymeric materials based
technique on their physico-chemical
followed by properties sustained the
M

coating with drug release.

Eudragit Ne 30D
and RS 30D
D

Captopril Minitablets Direct Only the system using [61]

compression Eudragit RL30D and
followed by combination of them as a
TE

coating gas-entrapped polymeric

membrane could float.
Eudragit RLPO
EP

Acyclovir Nanoparticles Nanoprecipitation As acyclovir: Eudragit [71]

technique RLPO ratio increased from
1:1.5 to 1:2, particle size
and drug entrapment
C

increased It also produced

sustain release.
AC

Cinnarizine Mucoadhesive Simplex lattice Eudragit RLPO and iron [62]

tablets design oxide combination showed
high level potential for
fabricating gastroretentive
as well as mucoadhesive
drug delivery systems.
Lercanidipine Gastroretentable Layering Patches prepared using the [63]
HCl mucoadhesive technique combination of Eudragit
patch RSPO and RLPO could
 ACCEPTED MANUSCRIPT

control the drug release up

to 12 h
Domperidone Bilayered Solvent casting Bilayered mucoadhesive [72]
mucoadhesive technique buccal patches with desired
buccal patches permeability could be
prepared
Metoprolol Solid dispersion Melting and RLPO showed higher [73]

PT
solvent method release than RSPO.
Verapamil Solid dispersion Direct The tablet containing [64]
hydrochloride compressed into a compression Eudragit RLPO has

RI
tablet extended the release rate
for 12 h
Promethazine Solid dispersions Coevaporation Eudragit RLPO [74]

SC
hydrochloride compressed into and coevaporates (1 : 5)
tablet coprecipitation displayed extended release
techniques of drug for 12 h
Eudragit RL100

U
Griseofulvin Polymer-coated Porous hollow Coated drug particles can [75]
drug fiber membrane- be potentially used for
AN
based antisolvent controlled release.
crystallization
Atazanavir Nanoparticles Nanoprecipitation To improve bioavailability [65]
M

method & in prolonged drug

release
Ibuprofen Tablet with Wet granulation Exploited successfully for [66]
D

interpolyelectrolyte colon-targeted delivery of

complexes ibuprofen
TE

(IPECs), formed
between Eudragit
RL100 (EL) and
chitosan (CS).
EP

Metformin Matrix tablet Wet granulation used to sustain drug [76]

hydrochloride technique release
Domperidone Buccal films Hot-melt improved bioavailability [67]
extrusion
C

Azithromycin Opthalmic inserts Modified solvent Prolonged release time and [68]
AC

casting method improved ocular

availability.
Lercanidipine Transdermal Solvent Drug release sustained upto [77]
hydrochloride patches evaporation 24 h.
technique
Sulfacetamide Nanosuspension Solvent Formulation of [78]
displacement sulfacetamide in Eudragit
method RL100 improve the
availability of
sulfacetamide at the
 ACCEPTED MANUSCRIPT

intraocular level.
Azelastine Microspheres Solvent Prolonged release of the [79]
hydrochloride evaporation drug over the period of
technique 6 hr.
Zidovudine Transdermal Solvent Increased permeation [80]
delivery evaporation
method

PT
Cloricromene Nanoparticle Quasi-emulsion Improves the shelf life and [81]
suspensions solvent diffusion bioavailability of this drug
technique after ophthalmic

RI
application
Eudragit RL 12,5
* * * * *

SC
*
No literature found

U
AN
M
D
TE
C EP
AC
 ACCEPTED MANUSCRIPT

Table 8, Reported Literature on Eudragit RS 30D, RSPO, RS 100 and RS 12,5

Drug name Dosage form/ Method of Application Refer

delivery Preparation ences
system
Eudragit RS 30D
Oxymatrine Osmotically Extrusion/ Gradual sustained release for [82]

PT
driven Pellets Spheronization 12 h
followed by fluid
bed coating

RI
Ambroxol Pellets Extrusion- Stable and sustain release [70]
hydrochloride spheronization formulation
technology followed

SC
by coating
Diclofenac Pellets Powder layering Retarded the drug release [87]
sodium technology and air rate and varied according to
suspension technique the type and amount of

U
plasticizers
Ketoprofen Pellets Extrusion and Eudragit RS 30 D has the [60]
AN
spheronisation effect to minimize the initial
followed by coating drug release but increase the
terminal drug release more
M

significantly.
Diclofenac Pellets Roto-agglomeration Eudragit RS 30 D provided [88]
sodium membranes successfully
controlling drug release over
D

an extended period of 24 h
Eudragit RSPO
TE

Propranolol Microballoons Non-aqueous O/O Drug release showed a [83]

hydrochloride emulsion solvent biphasic pattern with an
diffusion initial burst release, followed
EP

evaporation method by sustained release for 12 h

Alfuzosin Tablets Direct compression The release of Alfuzosin was [89]
hydrochloride prolonged for 20 h
Stavudine Microspheres Solvent evaporation Sustain release [90]
C

method
Ibuprofen Pellets Extrusion- Eudragit RLPO and RSPO [84]
AC

spheronization did not have a significant

effect on elastic modulus.
Lobenzarit Tablets Direct compression slower release rate [91]
disodium
Theophylline Microtablets Rotary tablet press Sustained-release [92]
Eudragit RS 100
Genistein Nanostructured Melt-emulsification 3.3-fold increase in corneal [85]`
lipid carrier technique penetration
(NLC)
 ACCEPTED MANUSCRIPT

Metformin HCl Bbilayer tablet Solvent evaporation Extended release of [93]

and Acarbose and cogrinding metformin HCl for 12 h from
techniques one layer
Verapamil Matrix tablet Wet granulation Coating with eudragit RS100 [94]
hydrochloride followed by method polymer minimized initial
coating burst release
Terbinafine positively Nanopreciptation Increased drug mean [95]

PT
hydrochloride charged method residence time and improved
controlled- its ocular bioavailability four
release fold.

RI
polymeric
Nanoparticles
as eye drop

SC
Lornoxicam matrix-type Solvent evaporation Sustain release and [86]
transdermal technique enhanced bioavailability
patch
Clotrimazole Bioadhesive Spray drying Controlled intravaginal drug [96]

U
Vaginal tablets technique release
containing
AN
microspheres
Eudragit RS 12,5
* * * * *
M

*
No literature found
D
TE
C EP
AC
 ACCEPTED MANUSCRIPT

Table 9, Patents on applications of Eudragit

S. Title of the Invention Patent Inventors Date Refer

No patent Number ences
1 Colonic The systems include US A.Andremont 05/2 [97]
delivery using pectin beads cross linked 2008012 H. Huguet 9/20
zn/pectin beads with zinc or any divalent 4279 08

PT
with a eudragit cation of interest, which
coating. beads are then coated with
Eudragit®-type polymers.

RI
2 Ursodeoxycholi The ursodeoxycholic acid- US J.H. Choy, 06/2 [98]
c acid-synthetic synthetic hydrotalcite- 2012015 G.E. Choi, 1/20
hydrotalcite- Eudragit hybrid was used 6263 M. C. Park, 12

SC
eudragit hybrid, for bitter-taste-blocking H. C. Chang
pharmaceutical effect and improved body
composition absorption rate with high
containing the solubility.

U
same and
method for
AN
preparing the
same
3 Modified Eudragit L100-55 for said US S. H. Amir 02/ [99]
M

release tablet pharmaceutical 2007010 C.E. Melissa 08/2

formulations formulation which 4782 007
with enhanced achieves a desired
D

mechanical hardness for tablets made

properties from the formulation.
TE

4 Curcuminoid Curcuminoid-eudragit US20140 H. Tummala, 09/1 [100]

complexes with complex, which enhance 271530 S. Kumar 8/20
enhanced the bioavailability of the 14
stability, curcumin component.
EP

solubility and/or
bioavailability
5 Improved Misoprostol was EP08968 C. David 09/2 [101]
stabilization of complexed with various 23 Tsay, R. Jen 5/20
C

misoprostol grades of Eudragit RS Lin Hue In 02

AC

series, Eudragit RL Lu Shu-bin

series, Eudragit S, Eudragi
t L. , The solid dispersions
were stable 6and showed
sustain release.
6 Sustained Controlled dissolution of EP03222 H. Stevens, 01/2 [105]
release the active principle 77 M. Chariot, 2/19
pharmaceutical independently of the pH, F. Arnold, 92
composition which consists of micro G. Lewis
particles containing the
 ACCEPTED MANUSCRIPT

active principle, coated

with a mixture of
ethylcellulose
and Eudragit RS.
7 Colonic Pectin beads are US A. 08/2 [106]
delivery of crosslinked with zinc ions 2008019 Andremont, 1/20
metallo- and the pectin beads are 9528 H. Huguet 08

PT
dependent coated with a Eudragit®
enzymes polymer.
8 Coated senna Senna extract with 20% WO/2011 P. H. Jorge 10.0 [102]

RI
extract granules sennosides are granulated /014976 2.20
with Eudragit L 100 and 11
then coated with Eudragit

SC
L 30 D 55
9 ketoprofen ketoprofen micro granules WO/2000 L. C. 11/0 [103]
microgranules, of eudragit RL and RS /064432 Marechal, 2/20
method for exhibited prolonged D.S.Pascal 00

U
preparing same release
and
AN
pharmaceutical
compositions
10 Formulation The polymeric base is US F. Robert, 01/1 [104]
M

stabilizer for cholestyramine- 2006001 R. Narayan, 9/20

proton pump OH, Eudragit EPO, 3880 Z. Joseph 06
inhibitors chitosan, or a mixture H. Ping
D

thereof. The composition

stabilizes the
benzimidazole derivative
TE

proton pump inhibitor in a

humid environment
11 Oral drug One active substance and US O. Isa 09/1 [107]
EP

delivery at least one coat 2015025 0/20

formulations comprising Eudragit E 0733 15
The formulation may be
used for releasing up to
C

about 55% of a total dose

as a loading dose in order
AC

to manage pain.
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RI
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