Formulation and Evaluation of

MUCOADHESIVE
DRUG DELIVERY
SYSTEMS
 Introduction
Novel drug delivery systems (NDDS)
are the system where the man searches
for new methods of entry of drugs in to the
body in order to show its activity in the
body .
The new drug delivery systems that
have been developed and developing are
the mucoadhesive drug delivery systems ,
drug patches, transdermal patches etc.
 Definition
Adhesion can be defined as the bond produced by contact
between a pressure - sensitive adhesive and a surface. The
American Society of testing and materials has defined it as the
state in which two surfaces are held together by interfacial
forces, which may consist of valence forces, interlocking
action or both.
Bioadhesion is defined as an ability of a material to adhere to
a biological tissue for an extended period of time
In the case of polymer attached to the mucin layer of a
mucosal tissue, the term “mucoadhesion” is used.
 Types of Drug delivery systems:
Depending upon the route of administration of the mucoadhesive drugs
they are different types .They are

1)Buccal delivery system

2)Sub lingual delivery system

3)Vaginal delivery system

4)Rectal delivery system

5)Nasal delivery system

6)Ocular delivery system

7)Gastro intestinal delivery system

Mechanism of
Mucoadhesion
Before discussing about the
mechanism of muco-
adhesion we must know
about the composition of
mucous briefly. Mucus is
composed mainly of
 Water (>95%)
 Glycoproteins of
exceptionally high
molecular weight
 Mineral salts -1 %
 Free proteins – 0.5 to 1%
Factors affecting Mucoadhesion
1. Polymer related factors

2.Environment related factors

3.Physiological factors

1. Polymer related factors

i) Molecular weight :
ii)Concentration of active polymer
iii)Flexibility of polymer chains

2.Environment related factors :

i)pH of polymer - substrate interface
ii) Applied strength
iii) Initial contact time
iv)Swelling

3. Physiological factors:

i)mucin trun over :

ii)Disease state

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Polymers
The following are the polymers their relative bio adhesive property

Polymer Bioadhesive property

 Carboxy methyl cellulose +++
 Hydroxyl propyl methyl cellulose +++
 Carbopol 934 +++
 Tragacanth +++
 Sodium alginate +++
 Polycarbophil +++
 Hydroxyl ethyl cellulose +++
 Gelatin ++
 Guar gum ++
 Gum karaya ++
 Pectin +
 Acacia +
 Polyvinyl pyrrolidone +

NOTE : +++ Excellent

++ Moderate
+ Poor
Advantages

Mucoadhesive dosage forms have three distinct advantages when

compared to conventional dosage forms

• 1)These dosage forms are readily localized in the region applied to

improve and enhance the bioavailability of drugs.

• 2)These dosage forms facilitate intimate contact of the formulation with

the underlying absorption surface. This allows modification of tissue
permeability for absorption of macromolecules ,such as peptides and
proteins. Inclusion of penetration enhancers such as Sodium
glycocholate, Sodium taurocholate and L-lysophosphotidyl choline
9LPC0 and protease inhibitors in the mucoadhesive dosage forms
resulted in better absorption of peptides and proteins.

• 3) Mucoadhesive dosage forms also prolong the residence time of the

dosage form at the site of application and absorption to permit once or
twice a day dosing.
Disadvantages
• Medications administered orally do not enter the blood stream immediately after
passage through the buccal mucosa. Instead they have to be swallowed and
then have to pass through a portion of the GIT before being absorbed. So the
action is not very rapid in the GIT as compared when the drug is administered
through buccal route.

• Certain drugs when ingested undergo drug destruction, there are several drugs
which are potentially in this category. Many drugs affect liver metabolism and
also cause destruction via first pass metabolism of other drugs.

• Oral ingestions results in more exposure of a drug to the GI tract. One of the
side effects of many antibiotics is the destruction of normal GI flora resulting in
diarrhea and overgrowth with dangerous organisms such as C. difficile.

• The absorption of mucoadhesive drugs is adversely affected by the presence of

food. Tetracyclines, in particular, complicates the administration of this class of
antibiotics via the oral route.

• Mucoadhesive drugs cannot bypass liver metabolism. Example, lipids can

directly interact with endogenous lipoproteins thus influencing blood lipid levels.
Different mucoadhesive
dosage forms
• Mucoadhesive Buccal Films:

Mucoadhesive buccal films are most commonly prepared by the solvent

casting technique in which various substrates including mercury, Teflon,
glass and aluminium are used for film formation. Among these
substrates, mercury was found to give best results.
• Mucoadhesive microspheres:

Mucoadhesive microspheres have advantages of efficient absorption and

enhanced bioavailability of drugs, a much more intimate contact with the
mucus layer, and specific targeting of drugs to the absorption site.
• Mucoadhesive microparticles:

Mucoadhesive microparticles is an improved drug delivery system which

are believed to bind to the mucus layer coating the stomach and other
regions of the GIT. These mucoadhesive microparticles bind to the
mucus layer leading either to slow release into the GIT or direct delivery
to the gastrointestinal mucosa.
• Mucoadhesive microcapsules:

Mucoadhesive microcapsules are a type of controlled-release

dosage form. They offer numerous benefits including reducing
stress resulting from restraint, handling, and dosing and
avoiding expensive or difficult drug administration procedures.
They can be used for vaginal administration to treat vaginal
infections and to increase patient convenience.
• Mucoadhesive tablets:

Mucoadhesive tablets have been developed to increase the

retention of drug in GIT and/or to keep a sustained release of
drug towards the medium from where it is constantly removed.
Thus, treatment of many diseases is done.
• Mucoadhesive patches:

These mucoadhesive formulations offer many advantages in

comparison to traditional treatments and can be proposed as a
new therapeutic tool against dental and buccal diseases and
disturbances.
Evaluation tests of muco-
adhesive tablets
• 1)Weight variation
• 2)Friability
• 3)Hardness
• 4)Content uniformity
• 5) Drug release study of Mucoadhesive tablets
• 6) Swelling index
• 7)Water sorption studies
• 8)Mucoadhesive strength
•
AIM AND OBJECTIVE
The objective of the DRUG CATEGORY CLASS HALF-LIFE
study mainly is to
develop, characterize
and evaluate Diltiazem Anti-anginal, Calcium 3-4.5 hours
mucoadhesive channel
dosage forms Anti-
employing various arrythmiatic blocking
mucoadhesive agent
polymers for Atenolol Anti- B-adrenergic 6-7 hours
prolonged Hypertensive,
absorption. blocking
• Anti-anginal agent
The mentioned drugs
are most commonly
used in the Nifedipine Anti- Calcium 2-5 hours
preparation of Hypertensive, channel
mucoadhesive drug
delivery systems. Anti-anginal blocking
agent
• Based on literature
survey, the best Captopril Anti- Acetylcholine 2-5 hours
excipients will be Hypertensive inhibitor
selected and the best Anti angial
method will be
followed to obtain
the final optimized
formulation.
 Rationality in the
selection of the
•
experiment
The rationality in carrying out the experiment is well approved
since, it is based on the selection of the optimal dose
involved. Mucoadhesive drugs have many properties which
make it rationally possible to carry out experiment on its
dosage forms. Its various advantages like increasing the
residence time of the drug, increasing the bioavailability and
contact time of drug are important to be studied and hence
build a platform for experimentation.
• Based on literature survey, by taking into account the various
physicochemical and pharmacokinetic properties of various
drugs, an optimal drug that can be employed in this
experiment is selected. Thus, selection of a drug by taking
into account mainly the half life value, solubility and
availability is carried out. Various procedures for the
formulation and evaluation of the selected drug are then
carried out resulting in the production, characterization and
evaluation of the finalized optimal product.
• Thus, the idea of selecting an optimal mucoadhesive dosage
form for experimentation after survey of literature of many
drugs is proved to be of great rationality.
Conclusion
The mucoadhesive drug delivery offers several advantages for controlled
drug delivery. The mucosa is well supplied with both vascular and lymphatic
drainage. The mucous membrane has a large surface area and is well
suited for a retentive device and appears to be acceptable to patients. With
the proper formulation and dosage form design, the permeability and the
local environment of the mucosa can be controlled and manipulated to
accommodate drug permeation. Mucoadhesive drug delivery is a promising
area for systemic delivery of orally inefficient drugs as well as an attractive
alternative for noninvasive delivery of potent peptide and perhaps protein
drug molecules. However, the need for safe and effective permeation and
absorption enhancers is a crucial component for a promising future in the
area of mucoadhesive drug delivery. A rational approach to dosage form
design requires a complete understanding of the physicochemical and
biopharmaceutical properties of the drug and excipients. Advances in
experimental and computational methodologies will be helpful in shortening
the processing time from formulation design to clinical use.
Literature survey
DRUGS CATEGORY POLYMERS DOSAGE FORM REFERENCE

Clotrimazole Anti-fungal Carbopol 934 Flims Indian journal of

&HPMC pharmaceutics
Vol 60 No. 1,
Jan-Feb 1998

Metronidazole Anti infective Ethyl cellulose tablets Journal of

pharmaceutical
research
Vol 7 No. 3,July
2008