FORMULATION CHARACTERIZATION AND EVALUATION OF NEW TOPICAL 5-FU BY DRUG ENTRAPMENT IN OLEIC ACID VESICLES.
Vipasha Dhillon1, Shiwang Sharma1, Subheet Jain2, Sandeep Arora1, Arvind Sharma1*
1. Chitkara College of Pharmacy, Chitkara University, Punjab.
2. Department of Pharmaceutical Sciences and Drug Research, Panjabi University, Patiala.
Due to the lower risk of systemic side effects topical treatment of skin disease appears favourable, yet the stratum corneum counteracts the penetration of xenobiotics into viable skin. Fatty acids have been widely used as adjuvant, vehicles in drug delivery viz penetration enhancers in topical delivery and in polymeric micelles to provide sustained release. However, the present investigation aims at exploring the potential of fatty acid vesicles for the topical delivery of 5-FU. Vesicles were prepared by film hydration method using oleic acid as a fatty acid principal component. Developed vesicles were characterized for size, size distribution, shape, In vitro release, pH dependent and storage stability, skin and ex-vivo skin permeation. Optical microscopy and TEM studies confirmed vesicular dispersion of fatty acid. The vesicles possessed higher entrapment efficiency (64.0±4.2%) with optimum vesicle size and homogeneity in regard to size distribution (PDI = 0.234 ± 0.016) at 7:3 oleic acid-to-5-FU ratio. In vitro drug release study suggested sustained release of drug from the vesicles. The vesicles were fairly stable at refrigerated conditions. Ex-vivo skin permeation and Confocal microscopic studies suggested that oleic acid vesicles penetrate the stratum corneum and retain the drug accumulated in the epidermal part of the skin. On the basis of sustained release behavior and skin retention it can be inferred that oleic acid vesicles can serve as a potential carrier for the topical localized delivery of bioactives.
Key words: Oleic acid, 5-FU, CLSM