Temperature-sensitive microemulsion gel: an effective topical delivery system for simultaneous delivery of vitamins C and E.
Microemulsions (ME)--nanostructured systems composed of water, oil, and surfactants--have frequently been used in attempts to increase cutaneous drug delivery. The primary objective addressed in this work has been the development of temperature-sensitive microemulsion gel (called gel-like ME), as an effective and safe delivery system suitable for simultaneous topical application of a hydrophilic vitamin C and a lipophilic vitamin E. By changing water content of liquid o/w ME (o/w ME), a gel-like ME with temperature-sensitive rheological properties was formed. The temperature-driven changes in its microstructure were confirmed by rotational rheometry, viscosity measurements, and droplet size determination. The release studies have shown that the vitamins' release at skin temperature from gel-like ME were comparable to those from o/w ME and were much faster and more complete than from o/w ME conventionally thickened with polymer (o/w ME carbomer). According to effectiveness in skin delivery of both vitamins, o/w ME was found the most appropriate, followed by gel-like ME and by o/w ME carbomer, indicating that no simple correlation between vitamins release and skin absorption could be found. The cytotoxicity studies revealed good cell viability after exposure to ME and confirmed all tested microemulsions as nonirritant.
Rozman
Branka
B
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, Askerceva 7, Ljubljana, Slovenia.
Zvonar
Alenka
A
Falson
Francoise
F
Gasperlin
Mirjana
M
D000279:Administration, Cutaneous; D000818:Animals; D001205:Ascorbic Acid / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004338:Drug Combinations; D004339:Drug Compounding; D004655:Emulsions; D005782:Gels; D006801:Humans; D007700:Kinetics; D009821:Oils / Q000737:chemistry* / Q000633:toxicity; D010316:Particle Size; D010539:Permeability; D012212:Rheology; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry* / Q000633:toxicity; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014783:Viscosity; D014810:Vitamin E / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D014815:Vitamins / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D014867:Water / Q000737:chemistry*
D004337:Drug Carriers; D004338:Drug Combinations; D004655:Emulsions; D005782:Gels; D009821:Oils; D013501:Surface-Active Agents; D014815:Vitamins; D014867:Water; D014810:Vitamin E; D001205:Ascorbic Acid