Preparation and evaluation of a buflomedil hydrochloride niosomal patch for transdermal delivery

J Liposome Res. 2015 Sep;25(3):191-201. doi: 10.3109/08982104.2014.974058. Epub 2014 Oct 30.

Abstract

Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery.

Objective: The present research work was aimed to develop niosomal-based transdermal buflomedil hydrochloride patch containing a stable formulation with improved drug permeation.

Materials and methods: Niosomes were prepared by solvent evaporation method using 32 factorial design. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. Optimized niosomal and liposomal formulation were loaded into a patch system. All the patches were then characterized for drug-excipient interaction study, scanning electron microscopy, pharmacotechnical properties and in vitro permeation studies.

Result: F9 formulation having optimum vesicle size (10.09 ± 1.2 µm), highest zeta potential (-85.4 ± 0.56 mV) and maximum percent entrapment efficiency (97.09 ± 0.11%) was selected as optimized formulation. In case of liposomes, formulation F12 was selected. Patches loaded with niosomes showed 95.12 ± 1.19% cumulative amount of drug permeated as compared to liposomal vesicle-loaded patches which showed 82.21 ± 1.24% and control patches 70.10 ± 1.33%.

Discussion: Flux, permeation rate and permeability coefficient were found to be higher in case of niosomal patches as compared to liposomal patches and control patches. Surfactant present in niosomes act as a penetration enhancer which contribute in the permeation enhancement of buflomedil hydrochloride from niosomes.

Conclusion: Thus, it was concluded that niosomal vesicles represented to be an efficient and stable vesicular carrier for transdermal delivery of buflomedil hydrochloride.

Keywords: Cholesterol; drug; flux; permeability; systemic circulation.