Penetration and distribution of three lipophilic probes in vitro in human skin focusing on the hair follicle

Fluorescent model substances of increasing lipophilicity (Oregon Green(R) 488, Bodipy(R), FL C-5 and Bodipy(R) 564/570 C-5) were selected to enable the visualization in the skin using confocal laser scanning microscopy. After measuring the penetration for 18 h, the nonfixed human scalp skin was imaged from the bottom parallel to the stratum corneum and in a cross-section view perpendicular to the skin surface. The images were evaluated by calculating relative accumulation values for different penetrants. The studies indicate that the penetrated amount is highest for Bodipy FL CS (medium lipophilicity) and lowest for Bodipy 564/570 CS (high lipophilicity) whereas Bodipy(R) 564/570 CS (high lipophilicity) reveals the highest relative accumulation in parts of the hair follicle compared to Oregon Green 488 (low lipophilicity). The addition of 30% (v/v) ethanol to the donor phase of substance with a low lipophilicity increases the follicular delivery. From our results we conclude that delivery to the hair follicle can be improved by increasing the drugs lipophilicity and optimizing the composition of the donor phase. However, no conclusion can be drawn about the actual route of transport to the hair follicle. (C) 2002 Elsevier Science B.V. All rights reserved.