Effect of vehicles and enhancers on the in vitro permeation of melatonin through hairless mouse skin.
The effects of vehicles and penetration enhancers on the in vitro permeation of melatonin through dorsal hairless mouse skin were investigated. Propylene glycol laurate (PGL), isopropyl myristate (IPM), propylene glycol monolaurate (PGML) and propylene glycol monocaprylate (PGMC) showed high permeation fluxes and PGL, PGML and PGMC decreased lag time significantly. In both of the binary co-solvents of diethylene glycol monoethyl ether (DGME)-PGL and DGME-IPM, the highest fluxes were achieved at 20% of DGME, which were 10.5 +/- 1.5 and 9.1 +/- 2.4 microg/cm2/h, respectively. Among fatty acids used as a permeation enhancer, capric acid and oleic acid in DGME-PGL (80:20 v/v) showed relatively high enhancing effects. Capric acid also shortened the lag time of melatonin from 2.4 +/- 0.7 to 1.3 +/- 0.2 h. Oleic acid, however, failed to shorten the lag time. Therefore, for effective solution formulations in terms of permeation flux and lag time, capric acid-containing DGME-PGL (80:20 v/v) could be used to enhance the skin permeation of melatonin.
Laboratory of Pharmaceutics, College of Pharmacy, Dongduk Women's University, Seoul, Korea.
Hye Sun
HS
Gwak
Seung Ung
SU
Kim
In Koo
IK
Chun
D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D008297:Male; D008550:Melatonin / Q000737:chemistry / Q000493:pharmacokinetics*; D051379:Mice; D008812:Mice, Hairless; D014677:Pharmaceutical Vehicles; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D012997:Solvents; D013268:Stimulation, Chemical
D000975:Antioxidants; D014677:Pharmaceutical Vehicles; D012997:Solvents; D008550:Melatonin