Design and evaluation of adapalene microemulsion for transfollicular drug delivery through guinea pig skin.

Abstract

Acne vulgaris can be treated topically with adapalene, a synthetic derivative of naphthoic acid with retinoid activity. Adapalene has a very low rate of percutaneous absorption and is almost completely insoluble in water. To obviate this problem, microemulsion (ME) carrier is used. The study's goals were to create and characterize adapalene-loaded ME and assess the drug's transfollicular route of penetration to see if hair follicles can serve as a conduit for the drug to enter the skin. Adapalene microemulsions (MEs) are made by combining the right amounts of the cosurfactant (propylene glycol), surfactant (Tween 80 and Span 20), and oil phase (oleic acid-Transcutol P (10:1)). Physical and chemical characteristics of MEs, including droplet size, stability, viscosity, drug release, and in vitro skin permeability via guinea pigs' hairy and non-hairy skin, were assessed. The range of 13.86-56.16 nm was found to be the average droplet size of ME formulations. The range of viscosities was 117-240 cps. The drug release profile reveals that 95.374 percent of the drug was released within the experiment's first 24 h. Compared to the adapalene control (aqueous suspension), all MEs enhanced the adapalene flow through both hairy and non-hairy skin. The surfactant/cosurfactant ratio had an impact on the amount of drug that passed through both skins because a larger ratio enhanced the adapalene affinity in the follicular route. Furthermore, the proportions of the water and oil phases in formulations, as well as the S/C ratio, have a significant impact on the physicochemical characteristics and adapalene permeability across both pathways.