IngentaConnect Niosomal delivery of 5-fluorouracil

Abstract:

Non-ionic surfactant vesicles (niosomes) have shown promise as cheap, chemically stable alternatives to liposomes. Niosomes of spans (Sorbitan monoesters) have shown promise of commercial exploitation. Hence, niosomes were prepared of 5-fluorouracil (FU) using different spans. Niomsomes were prepared bythehand shakingmethod (HSM), reversephaseevaporation(REV) and ether injection method (EIM) using a series of Spans, i.e. Span 20, 40, 60 and 80. HSM giving least permeable vesicles were used to study the effect of variables like type of Span, composition of lipid and total lipid concentration on entrapment efficiency (EE) and release rate. Span 40 and 60 released 40.9 and 37.1%drug in 6h while Span 20 and 80 displayed 52.2 and 57.1%release, respectively in the same time. Niosomes of Span 40 showed amean vesicle size of 8.1mum, EE of 15:3 1:3%and released 78.6% drug in 6h; inclusion of cholesterol reduced the vesicle size to4.8mum, EE to12:3 0:9%and the release to 50.5%(in 6h), while incorporation of dicetyphosphate further reduced the vesicle size to3.87mum, EE to10:9 1:1%and reduced release to40.9%(in 6h). Increase in the amount of lipid used translated intoan almost linear increase in EE. Biodistribution of drug in rats was modified on encapsulation. The concentration of niosomal drug in liver, lung and kidney was increased while it decreased in intestine compared to free drug solution following intravenous administration. The niosomal formulation displayed higher and sustained plasma drug level profile compared to free drug solution. Pharmacokinetic calculations revealed an increase in half-life, area under the curve and decrease in volume of distribution of the drug on encapsulation. Thus, the study suggests that niosomes can act as promising carriers for 5-Fluorouracil.

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