Microemulsion and Microporation Effects on the Genistein Permeation Across Dermatomed Human Skin

• Published in: AAPS PharmSciTech Vol. 19; no. 8; pp. 3481 - 3489
• Main Authors: Chen, Li, Annaji, Manjusha, Kurapati, Sharmila, Ravis, William R., Jayachandra Babu, R.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.11.2018
• Subjects: Administration, Cutaneous; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Drug Compounding; Emulsions; Genistein - pharmacokinetics; Humans; Permeability; Pharmacology/Toxicology; Pharmacy; Research Article; Skin - metabolism; Skin Absorption; Surface-Active Agents - chemistry; Theme: Advances in Topical Delivery of Drugs; drug delivery, permeation; microemulsion; Genistein; human skin
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-018-1150-9

This study reports the microemulsion (ME) effects on the permeation of genistein across normal (intact) and microporated human skin. The genistein formulation was optimized to know the stable ME region in the pseudo-ternary phase diagrams and to maximize the skin permeation and retention of genistein. The phase diagrams were constructed with different oil phases, surfactants, and their combinations. The influence of formulation factors on the permeation through intact and microporated human skin was determined. Based on its wide ME region, as well as permeation enhancement effects, oleic acid was used as an oil phase with various surfactants and co-surfactants to further maximize the ME region and skin permeation. The water content in the formulation played an important role in the ME stability, droplet size, and flux of genistein. For example, the ME with 20% water exhibited 4- and 9-fold higher flux as compared to the ME base (no water) and aqueous suspension, respectively. Likewise, this formulation had demonstrated 2- and 4-fold higher skin retention as compared to the ME base (no water) and aqueous suspension, respectively. The skin microporation did not significantly increase the skin permeation of genistein from ME formulations. The ME composition, water content, and to a lesser extent the ME particle size played a role in improving the skin permeation and retention of genistein.