NIOSOMES - a carrier based drug delivery

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seminar on NIOSOMES :





INTRODUCTION Niosomes are a novel drug delivery system, in which the medication is encapsulated in a vesicle. The niosomes are very small, and microscopic in size. Their size lies in the nanometric scale. Niosomes are unilamellar or multilamellar vesicles .The vesicle is composed of a bilayer of non-ionic surface active agents and hence the name niosomes.

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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:

Structure of Niosomes Head part Drug molecules Tail part Phospo-lipids

Antibody Attachment:

Antibody Attachment

 Advantages :

Advantages 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:

Method of preparation Etherinjection method Hand shaking method Sonication Multiple membrane extrusion method Reverse Phase Evaporation Technique Aqueous Dispersion Method

A. Etherinjection method :

A. Etherinjection method Introduce a solution of surfactant dissolved in diethyl ether into warm water maintained at 60°C. Surfactant mixture in ether is injected through 14-gauge needle into an aqueous solution of material. 14-gauge needle

B .  Hand shaking method:

B . Hand shaking method 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 0-60°C with gentle agitation ROTARY EVAPORATOR

C. Sonication :

C. Sonication Aliquot of drug solution in buffer is added to surfactant/cholesterol mixture in a 10-ml glass vial. Mixture is probe sonicated at 60°C for 3 minutes using a sonicator with a titanium probe to yield niosomes. Sonicator

D. Multiple membrane extrusion method:

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 MEMBRANES

E. Reverse Phase Evaporation Technique :

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 4-5°C. organic phase is removed at 40°C under low pressure The resulting viscous niosome suspension is diluted with PBS and heated on a water bath at 60°C for 10 min to yield niosomes. F. Aqueous Dispersion Method Micro dispersion of containing solute for encapsulation Controlled temp. and agitation provides vesicles

Recently Advanced Techniques:

Recently Advanced Techniques Bubble Method Formation of niosomes from proniosomes

Separation of Unentrapped drug:

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. Dialysis Machine

2. Gel Filtration:

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. Gel filtration

Gel Filtration:

Gel Filtration

3. Centrifugation:

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. centrifuser

Characterization of Niosomes :

Characterization of Niosomes A.Entrapment Efficiency Entrapment efficiency = (Amount entrapped total amount) x 100 Encapsulation efficiency and Solute release rates. Factors Effect of cholesterol Nature of hydrophilic head group Nature of alkyl side chain. Nature of encapsulated solute Vesicle surface charge

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B. Vesicle Morphology Light Microscopy Photon Correlation Microscopy Freeze Fracture Electron Microscopy Co focal laser scanning Microscopy SEM TEM C. In-vitro release

Factors affecting vesicles size, entrapment efficiency and release characteristics:

Factors affecting vesicles size, entrapment efficiency and release characteristics Drug Amount and type of surfactant Cholesterol content Methods of preparation

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Diagramatic representation

Stability of niosomes:

Stability of niosomes Stability in buffer Stability in hypertonic media . osmotic shrinkage. Stability in hypotonic media. Stability in vivo . plasma component interaction

Marketed Products :

Marketed Products Lancôme has come out with a variety of anti-ageing products which are based on noisome formulations. L’Oreal is also conducting research on anti-ageing cosmetic products.


Applications 1) Targeting of bioactive agents To reticulo-endothelial system To organs other than RES 2) Neoplasia Doxorubicin Niosomal delivery of Doxorubicin to mice bearing S-180 tumor increased their life span and decreased the rate of proliferation of sarcoma 3) Leishmaniasis 4) Delivery of peptide drugs Oral delivery of 9-desglycinamide, 8-arginine vasopressin entrapped in niosomes increase stability of peptide significantly.

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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

Conclusion :

Conclusion The concept of incorporating the drug into niosomes for a better targeting of the drug at appropriate tissue destination . They presents a structure similar to liposome and hence they can represent alternative vesicular systems with respect to liposomes 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 , parental, etc.


REFERENCES Vyas S.P. , Khar R.K. ,Targeted & Controlled Drug Delivery, Novel Carrier Systems, CBS Publication ,2002 ,Page No.249-279 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; R1-R3: 61.

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