Wednesday, May 14, 2008

Niosomes

Liposomes have following members in its family:
2. Virosomes
3. Niosomes
4. Archaeosomes
6. Cochleates
7. Proteosomes (Gideon F. A. Kersten et al.)

Introduction of Niosomes:
Niosomes are unilamellar or multilamellar vesicles [3] which are very similar to liposomes in structure, prepared primarily from non-ionic surfactant vesicles. They are one of the most studied alternative to liposomes. Niosomes can be changed or modified by the incorporation of other excipients like cholesterol, into the membrane and they can possess one or more lipid bilayers encapsulating an aquous core. A diverse range of materials have been used to form niosomes such as sucrose ester surfactants and polyoxyethylene alkyl ether surfactants. [1]

(D. Paolina) Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. (R. M. Handjani-Vila et al.)In comparison with classical formulations such as emulsions, these systems exhibit lower toxicity and permit closer control of the availability of active substances at the stratum corneum.

Preparation of Niosomes:

(A. J. Baillie et al.) Vesicles were prepared on hydration of a mixture of a single or double alkyl-chain, non-ionic surfactant with cholesterol. These vesicles, or 'niosomes', are capable of entrapping and retaining water soluble solutes such as carboxyfluorescein, are osmotically active and can be formulated to release entrapped solute slowly.

Properties of Niosomes:
There is good entrapment efficiency in niosomes. (T. Yoshioka et al.)There is increased efficiency of entrapment of molecules with increasing cholesterol content. Studies show that (Maria Manconi et al.) small, niosomal formulations,(which are saturated with tretinoin) charged negatively, give higher cutaneous drug retention than both liposomes and commercial formulation in the area of study.

This is one of the representation of the Niosome. Here "o" represents "Hydrophilic head group"and "--" represents "Hydrophobic tail"

Characteristics of the head and tail groups:


Hydrophilic head may consist of the following groups:

1. Ethylene Oxide head groups
2. Polyhydroxy head groups
3. Glycerol head groups
4. Crown ether head groups
5. Sugar head groups i.e. Mannose, lactose, glucose, galactose

Hydrophobic tail may consist of the following groups:
1. Perfluoroalkyl surfactants that form vesicles having chain lengths as short as C10
2. One or two alkyl or perfluoroalkyl groups or in certain cases a single steroidal group.
3. Additionally crown ether amphiphiles bearing a steroidal C14 alkyl or C16 alkyl hydrophobic unit have been shown to form vesicles
4. Alkyl group chain length is usually from C12-C18 (one, two or three alkyl chains).
Preference of Niosomes over liposomes:
Niosomes are now preferable on liposomes as
1. They have more stability
2. Different grades of purity in respect of phospholipids and
3. Low cost
4. Non-ionic surfactants can be easily stored

(Ijeoma F. Uchegbu et al.)Following factors affect the Physico-Chemical properties of Niosomes:
1. Choice of surfactants and main or membrane additives.
2. Temperature.
3. Hydration.
4. Size reduction techniques.
5. Natural properties of drugs.

Niosomes are also affected by Addition of kinetic energy which is affected by size reduction techniques.

Different Niosomes:

1. Bola-Surfactant containing niosomes:
(D. Paolino et al.)Niosomes made of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol (2:3:1 molar ratio) are named as Bola-Surfactant containing niosomes.
2. Proniosomes:
(Chengjiu Hu et al.)A dry product which may be hydrated immediately before use to yield aqueous niosome dispersions. These ‘proniosomes’ minimize problems of niosome physical stability such as aggregation, fusion and leaking, and provide additional convenience in transportation, distribution, storage, and dosing.
In short;
1. Carrier + Surfactants = Proniosomes
2. Proniosomes + H2O = Niosomes
(Adnan Azeem et al.)In case of Frusemide delivery in the body, it has been found that proniosomal formulations have been found effective to sustain the level of drug in the blood.

Uses of Niosomes:
(H. Schreier et al.) Topical liposomes or niosomes may serve
1. as solubilization matrix,
2. as a local depot for sustained release of dermally active compounds,
3. as penetration enhancers,
4. or as rate-limiting membrane barrier for the modulation of systemic absorption of drugs.

(Rita Muzzalupo et al.)Niosomes have shown promise as cheap and chemically stable drug delivery systems. Various uses of Niosomes include Transdermal applications. They cause enhanced delivery of drugs through stratum corneum. Niososmes are also increasingly used for the ocular delivery of drugs for the topical treatment of glaucoma. The niosomal application of both antigens and DNA encoding for antigens results in an enhancement of the humoral and cellular immune response to the said antigens. [2]

Scientists (Donatella Paolino et al.) are researching for topical delivery system by niosomes for 5-fluorouracil (5-FU), largely used in the treatment of different forms of skin cancers.

References:
Transdermal and Topical Drug Delivery: From Theory to Clinical Practice by Adrian C. Williams

Nanoparticulates As Drug Carriers by Vladimir P. Torchilin

Synthetic Surfactant Vesicles: Niosomes and Other Non-Phospholipid Vesicular Systems (Drug Targeting and Delivery) by L. F. Uchegu

Adnan Azeem, Nilu Jain; Zeenat Iqbal; Farhan Jalees Ahmad; Mohammad Aqil; Sushama Talegaonkar, Feasibility of Proniosomes-Based Transdermal Delivery of Frusemide: Formulation Optimization and Pharmacotechnical Evaluation. Pharmaceutical Development and Technology, Volume 13, Issue 2, March 2008 , pages 155 - 163
A. J. Baillie, A.T. Florence , L. R. Hume , G. T. Muirhead , A. Rogerson. The preparation and properties of niosomes--non-ionic surfactant vesicles. The Journal of Pharmacy and Pharmacology. 1985 Dec; 37(12): Pages 863-8.

Chengjiu Hu, David G. Rhodes. Proniosomes: A Novel Drug Carrier Preparation. International Journal of Pharmaceutics, Volume 185, Issue 1, 5 August 1999, Pages 23-35

Donatella Paolino, Donato Cosco, Rita Muzzalupo, Elena Trapasso, Nevio Picci and Massimo Fresta, Innovative bola-surfactant niosomes as topical delivery systems of 5-fluorouracil for the treatment of skin cancer. International Journal of Pharmaceutics, Volume 353, Issues 1-2, 2 April 2008, Pages 233-242

D. Paolino, R. Muzzalupo, A. Ricciardi, C. Celia, N. Picci, M. Fresta. In vitro and in vivo evaluation of Bola-surfactant containing niosomes for transdermal delivery. Biomedical Microdevices. 2007 Aug;9(4): Pages 421-33.
Gideon F. A. Kersten, Daan J. A. Crommelin, Liposomes and ISCOMs. Vaccines, Volume 21, Issues 9-10, 14 February 2003, Pages 915-920

H. Schreier, J. Bouwstra. Liposomes and niosomes as topical drug carriers : dermal and transdermal drug delivery. Journal of Controlled Release 1994, vol. 30, no1, Pages 1-15.

Ijeoma F. Uchegbu, Suresh P. Vyas, Non-ionic surfactant based vesicles (niosomes) in drug delivery. International Journal of Pharmaceutics 172 (1998) Pages 33–70.

Maria Manconi,Chiara Sinico, Donatella Valenti, Francesco Lai and Anna M. Fadda, Niosomes as carriers for tretinoin III. A study into the in vitro cutaneous delivery of vesicle-incorporated tretinoin. International Journal of Pharmaceutics, Volume 311, Issues 1-2, 27 March 2006, Pages 11-19

R. M. Handjani-Vila, A. Ribier, B. Rondot and G. Vanlerberghie. Dispersions of lamellar phases of non-ionic lipids in cosmetic products. International Journal of Cosmetic Science, Volume 1 Issue 5 Page 303-314, October 1979

Rita Muzzalupo, Fiore Pasquale Nicoletta, Sonia Trombino, Roberta Cassano, Francesca Iemma and Nevio Picci. A new crown ether as vesicular carrier for 5-fluoruracil: Synthesis, characterization and drug delivery evaluation. Colloids and Surfaces B: Biointerfaces, Volume 58, Issue 2, 1 August 2007, Pages 197-202.

T. Yoshioka, B. Sternberg, A. T. Florence, Preparation and properties of vesicles (niosomes) of sorbitan monoesters (Span 20, 40, 60 and 80) and a sorbitan triester (Span 85). International journal of pharmaceutics, 1994, vol. 105, no1, Pages 1-6.



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