In vitro skin absorption and drug release - a comparison of six commercial prednicarbate preparations for topical use.
Reconstructed human epidermis is a useful tool for in vitro skin absorption studies of chemical compounds. If this may hold true also for topical dermatics, we investigated the glucocorticoid prednicarbate applied by two sets (innovator and generic) of cream, ointment and fatty ointment using the commercially available EpiDerm model. Moreover, stability and local tolerability of the preparations as well as drug release were studied, to estimate an influence on prednicarbate absorption and metabolism. While release ranked in the order cream<fatty ointment<ointment for both sets of preparations, prednicarbate penetration and permeation of the EpiDerm model did not. Less PC uptake observed with the generic ointment and fatty ointment appeared to be linked to impaired enzymatic ester cleavage within the tissue. Thus with drugs subject to skin metabolism, cutaneous uptake is not to be derived from drug release studies, yet has to be studied experimentally with viable skin or reconstructed human epidermis.
Lombardi Borgia
S
S
Institut für Pharmazie (Pharmakologie und Toxikologie), Freie Universität Berlin, Berlin, Germany.
Schlupp
P
P
Mehnert
W
W
Schäfer-Korting
M
M
D000287:Administration, Topical; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D066298:In Vitro Techniques; D008954:Models, Biological; D011239:Prednisolone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D012869:Skin Absorption
D011239:Prednisolone; C035287:prednicarbate