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y Niosomes are non-ionic surfactant vesicles obtained

on hydration of synthetic nonionic surfactants, with or without incorporation of cholesterol or other lipids. y They are vesicular systems similar to liposomes that can be used as carriers of amphiphilic and lipophilic drugs y It is less toxic and improves the therapeutic index of drug by restricting its action to target cells

y Niosomes are a novel drug delivery system, in which the medication is

encapsulated in a vesicle.
y The niosomes are very small, and microscopic in size. Their size lies in the

nanometric scale.
y Niosomes are unilamellar or multilamellar vesicles.The vesicle is composed of

a bilayer of non-ionic surface active agents and hence the name niosomes.
y A diverse range of materials have been used to form niosomes such as sucrose

ester surfactants and polyoxyethylene alkyl ether surfactants, alkyl ester, alkyl amides, fatty acids and amino acid compound.

Structure of Niosomes
y Niosomes are microscopic lamellar structures which are formed on the admixture of non-

ionic surfactant of the alkyl or dialkyl polyglycerol ether class and cholesterol with subsequent hydration in aqueous media.

y The bilayer in the case of niosomes is made up of non-ionic surface active agents rather than

phospholipids as seen in the case of liposomes.

y Most surface active agents when immersed in water yield micellar structures, however some

surfactants can yield bilayer vesicles which are niosomes. Niosomes may be unilamellar or multilamellar depending on the method used to prepare them.

y The niosome is made of a surfactant bilayer with its hydrophilic ends exposed on the outside

and inside of the vesicle, while the hydrophobic chains face each other within the bilayer.

y Hence, the vesicle holds hydrophilic drugs within the space enclosed in the vesicle, while

hydrophobic drugs are embedded within the bilayer itself.

y The figure below will give a better idea of what a niosome looks like and where the drug is located

within the vesicle

Comparison of Niosomes v/s Liposomes

y Niosomes are different from liposomes in that they offer certain advantages over liposomes. y Liposomes face problems such as they are expensive, their ingredients like phospholipids

are chemically unstable because of their predisposition to oxidative degradation, they require special storage and handling and purity of natural phospholipids is variable.

y Niosomes do not have any of these problems. Also since niosomes are made of uncharged

single-chain surfactant molecules as compared to the liposomes which are made from neutral or charged double chained phospholipids, the structure of niosomes is differentfrom that of liposomes.

y However Niosomes are similar to liposomes in functionality. Niosomes also increase the

bioavailability of the drug and reduce the clearance like liposomes.

y Niosomes can also be used for targeted drug delivery, similar to liposomes. As with

liposomes, the properties of the niosomes depend both- on the composition of the bilayer, and the method of production used.

y Drug targeting can be defined as the ability to direct a therapeutic agent specifically to desired site

of action with little or no interaction with nontarget tissue. y In niosomes, the vesicles forming amphiphile is a non-ionic surfactant such as Span 60 which is usually stabilized by addition of cholesterol and small amount of anionic surfactant such as dicetyl phosphate.

Advantages of Niosomes
y The vesicle suspension being water based offers greater patient

compliance over oil based systems y Since the structure of the niosome offers place to accommodate hydrophilic, lipophilic as well as ampiphilic drug moieties, they can be used for a variety of drugs. y The characteristics such as size, lamellarity etc. of the vesicle can be varied depending on the requirement. y The vesicles can act as a depot to release the drug slowly and of controlled release. Other advantages of niosomes are: y They are osmotically active and stable. y They increase the stability of the entrapped drug y Handling and storage of surfactants do not require any special conditions y Can increase the oral bioavailability of drugs

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Can enhance the skin penetration of drugs They can be used for oral, parenteral as well topical use The surfactants are biodegradable, biocompatible, and non-immunogenic Improve the therapeutic performance of the drug by protecting it from the biological environment and restricting effects to target cells, thereby reducing the clearance of the drug. The niosomal dispersions in an aqueous phase can be emulsified in a nonaqueous phase to control the release rate of the drug and administer normal vesicles in external non-aqueous phase. High patient compliance in comparison with oily dosage forms. Accommodate drug molecules with a wide range of solubilities. Characteristics of the vesicle formulation are variable and controllable Osmotically active and stable, as well as they increase the stability of entrapped drug. Biodegradable, biocompatible and nonimmunogenic.

Method of preparation
A. Ether injection method Introduce a solution of surfactant dissolved in diethyl ether into warm water maintained at 60C. Surfactant mixture in ether is injected through 14-gauge needle into an aqueous solution of material. B . Hand shaking method (Thin film hydration technique) Surfactant and cholesterol are dissolved in a volatile organic solvent Organic solvent is removed at room temperature using rotary evaporator leaving a thin layer of solid mixture deposited on the wall of the flask Dried surfactant film can be rehydrated with aqueous phase at 0-60C with gentle agitation

C . Sonication Aliquot of drug solution in buffer is added to the surfactant/cholesterol mixture in a 10-ml glass vial Mixture is probe sonicated at 60C for 3 minutes using a sonicator with a titanium probe to yield niosomes. D. Multiple membrane extrusion method Mixture of surfactant, cholesterol and dicetyl phosphate in chloroform is made into thin film by evaporation The film is hydrated with aqueous drug solution and the resultant suspension extruded through polycarbonate membranes

E. Reverse Phase Evaporation Technique Cholesterol and surfactant (1:1) are dissolved in a mixture of ether and chloroform. An aqueous phase containing drug is added to this and the resulting two phases are sonicated at 4-5C. organic phase is removed at 40C under low pressure The resulting viscous niosome suspension is diluted with PBS and heated on a water bath at 60C for 10 min to yield niosomes. F. Aqueous Dispersion Method Microdispersion of containing solute for encapsulation Controlled temp. and agitation provides vesicles

Recently Advanced Techniques

y Bubble Method y Formation of niosomes from proniosomes

Table 1: Drugs incorporated into niosomes by various methods

Method of preparation Drug incorporated

Ether Injection

Sodium stibogluconate (14,20) Doxorubicin (21)

Hand Shaking

Methotrexate (12) Doxorubicin (21)


9-desglycinamide 8-arginine Vasopressin Oestradiol(5,19)

Separation of Unentrapped Drug

1. Dialysis The aqueous niosomal dispersion is dialyzed in a dialysis tubing against phosphate buffer or normal saline or glucose solution. 2. Gel Filtration The unentrapped drug is removed by gel filtration of niosomal dispersion through a Sephadex-G-50 column and elution with phosphate buffered saline or normal saline. 3. Centrifugation The niosomal suspension is centrifuged and the supernatant is separated. The pellet is washed and then resuspended to obtain a niosomal suspension free from unentrapped drug.

Characterization of Niosomes
A. Entrapment Efficiency Entrapment efficiency = (Amount entrapped total amount) x 100 B.Vesicle Morphology Light Microscopy Photon Correlation Microscopy Freeze Fracture Electron Microscopy Confocal laser scanning Microscopy SEM TEM C. In-vitro release

Factors affecting vesicles size, entrapment efficiency and release characteristics

y Drug y Amount and type of surfactant y Cholesterol content y Methods of preparation

Marketed Products
y Lancome has come out with a variety of anti-ageing products

which are based on niosome formulations. LOreal is also conducting research on anti-ageing cosmetic products.

1) Targeting of bioactive agents a) To reticulo-endothelial system b) To organs other than RES 2) Neoplasia Doxorubicin Niosomal delivery of bearing S-180 tumor increased their the rate of proliferation of sarcoma 3) Leishmaniasis 4) Delivery of peptide drugs Oral delivery of 9-desglycinamide, entrapped in niosomes increase significantly.

Doxorubicin to mice life span and decreased

8-arginine vasopressin stability of peptide

5) Immunological application of niosomes enhance the antibody production in response to bovine serum albumin 6) Niosomes as carriers for Hemoglobin 7) Transdermal delivery of drugs by niosomes e.g. erythromycin

y The concept of incorporating the drug into niosomes for a

better targeting of the drug at appropriate tissue destination . y They presents a structure similar to liposome and hence they can represent alternative vesicular systems with respect to liposomes y Niosomes are thoughts to be better candidates drug delivery as compared to liposomes due to various factors like cost, stability etc. Various type of drug deliveries can be possible using niosomes like targeting, ophthalmic, topical, parentral, etc.

y Vyas S.P. , Khar R.K. ,Targeted & Controlled Drug Delivery,

y y

y y

Novel Carrier Systems, CBS Publication ,2002 ,Page No.249279 Malhotra M. and Jain N.K. Niosomes as Drug Carriers. Indian Drugs 1994, Page No: 81-86. Chandraprakash K.S., Udupa N., Umadevi P. and Pillai G.K. Pharmacokinetic evaluation of surfactant vesicles containing methotrexate in tumor bearing mice. Int. J. Pharma. 1990; R1R3: 61.