Formulation and evaluation of a transfersomal vesicular carrier system for enhanced topical delivery of NIPRD-AF1

Abstract

The potentials of transfersomal formulations for transdermal delivery of NIPRD-AF1 was investigated. NIPRD-AF1 is a phytomedicine derived from the leaves of an indigenous plant, for use in the treatment of fungal infections. A transfersomal vesicular carrier system of NIPRD-AF1 was formulated and evaluated for topical application. Transfersomes of AF1 were prepared by solvent evaporation method using a phospholipid (Phospholipon 90 H) and varying concentrations of a mixture of surfactants (sodium lauryl sulphate, sorbitan monolaurate and Tween 80), and other performance enhancing excipients. The ointment was prepared by the fusion method using British Pharmacopoeia (BP) standard. The transfersomal carrier system was characterized using vesicle morphology, pH, entrapment efficiency (EE) and stability. The in vitro drug release of the transfersomes were studied using rat skin and Franz diffusion cell and compared to that of the ointment formulation of AF1. Transfersome formulation with the highest concentration of phospholipon and surfactants had optimal characteristics with an entrapment efficiency of 76.4 ± 0.04%. Optical microscopy showed presence of spherical vesicles in the transfersomal formulation with mean size (diameter) range of 57.5 ± 2.4 – 79.5 ± 3.10 μm. The pH values ranged between 6.40 and 6.48. The stability study showed that the transfersome formulations were most stable between 4-8^oC. All the transfersomal formulations showed potentials for systemic delivery and better permeation profiles than the ointment formulation of AF1.

Keywords: NIPRD-AF1, transfersome, ointment, permeation, transdermal drug delivery