Preparation and in vivo evaluation of lecithin-based microparticles for topical delivery of minoxidil

• Published in: Archives of pharmacal research Vol. 40; no. 8; pp. 943 - 951
• Main Authors: Lee, Hyo-Jung, Oh, Dong-Won, Na, Min-Ju, Kim, Dong-Wook, Yuk, Dong-Yeon, Choi, Hyoung-Chul, Lee, Yong-Beom, Han, Kun, Park, Chun-Woong
• Format: Journal Article
• Language: English
• Published: Seoul Pharmaceutical Society of Korea 01-08-2017; 대한약학회
• Subjects: Administration, Cutaneous; Alopecia - drug therapy; Animals; Drug Carriers - chemistry; Drug Delivery Systems; Female; Hair - drug effects; Hair - growth & development; Humans; Lecithins - chemistry; Male; Medicine; Mice; Mice, Inbred C57BL; Microspheres; Minoxidil - administration & dosage; Minoxidil - pharmacokinetics; Minoxidil - pharmacology; Pharmaceutical Solutions; Pharmacology/Toxicology; Pharmacy; Rats; Rats, Sprague-Dawley; Research Article; Skin Absorption; Vasodilator Agents - administration & dosage; Vasodilator Agents - pharmacokinetics; Vasodilator Agents - pharmacology; 약학; Skin irritation; Skin horniness; Lecithin; Minoxidil; Hair growth
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-017-0934-x

Minoxidil is widely used for treatment of androgenic alopecia. Commercial products containing minoxidil are usually in solution form. Repeated applications of minoxidil solution can lead to adverse effects such as skin irritation and horniness. The aims of this study were to prepare lecithin-based microparticle in minoxidil solution for enhancement of minoxidil topical delivery and skin protection and evaluate the ability of lecithin on in vitro delivery, in vivo hair growth, and skin trouble improvement compared to commercial minoxidil solution. In in vitro skin permeation study, minoxidil solution containing lecithin microparticle showed higher skin penetration rate and higher retention of drug inside the skin compared to minoxidil solution without lecithin. After topical application of minoxidil solutions with or without lecithin to C57BL/6 mice, minoxidil 5% solution containing lecithin microparticle showed hair re-growth as efficient as commercial product of minoxidil 5% solution. It also significantly improved skin troubles while commercial product presented horny substance and crust formation. Therefore, the lecithin-based microparticle in minoxidil 5% solution has good ability to promote hair growth without adverse effects.