Effect of lipid and edge activator concentration on development of aceclofenac-loaded transfersomes gel for transdermal application: <i>in vitro</i> and <i>ex vivo</i> skin permeation
Narendar Dudhipala, Riyaz Phasha Mohammed, Ahmed Adel Ali Youssef, Nagaraj Banala
Abstract
The present investigation focused mainly on the development of aceclofenac (AF) loaded transfersomal gel (AF-TG) to minimize the frequency of oral dosing during the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. AF-loaded transfersomes (AF-TS) were prepared by using the film hydration method. The effect of drug loading, pH of hydration medium, edge activator (EA) and lipid concentration on the properties of the AF-TS were studied and optimized. Optimized AF-TS converted into AF-TG by the addition of carbopol 934. Morphology and compatibility studies of AF-TS were observed with scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). AT-TG formulation was evaluated further for ex vivo skin permeation studies compared with marketed Hifenac 30 g gel. Optimized AF-TS showed vesicle size, PDI, and zeta potential of 111.1 ± 3.2 nm, 0.19 ± 0.02, and −29.6 ± 1.2 mV, respectively. Entrapment efficiency of 74.1 ± 1.8% with pH 5.8 phosphate buffer as a hydration medium and 17.1 ± 0.9 elasticity at 0.15%w/v EA and 1%w/v lipid concentration were observed. SEM and DSC studies revealed the spherical shape and no incompatibilities in the AF-TS formulation. The permeability of the AF from AF-TG was enhanced by 14-folds with similar rheological properties compared with marketed gel. Overall, TG containing AF was superior to marketed AF gel formulation for enhanced skin delivery. Therefore, TS and TG formulation could be considered as an alternative delivery approach for the enhanced transdermal application of AF.