Different approaches for improving skin accumulation of topical corticosteroids.
The aim of this paper was to evaluate the effect of vehicle, chemical enhancer and iontophoresis on the skin accumulation of clobetasol propionate (CP) and mometasone furoate (MF). In vitro permeation experiments were performed using pig ear skin as barrier and HPLC as quantification method. The formulations tested were chitosan gels, sodium-deoxycholate gels and commercial creams of CP and MF. The results obtained indicate that Na-DOC gel had an enhancing effect on the skin accumulation of both active agents. This effect was more evident with CP especially in the stratum corneum and epidermis which are the target sites of topical steroidal treatment. Two terpene derivatives (D-limonene and nerolidol) and Transcutol P were evaluated as chemical penetration enhancers. Nerolidol produced considerable increase in the amount of CP and MF accumulated without any permeation across the skin. The application of electric current (anodal iontophoresis) to the gels improved the accumulation of MF while it did not effect the accumulation of CP. Due to the best accumulation results of nerolidol, the enhancement effect in combination with iontophoresis was also investigated. It was shown that, the combination of anodal iontophoresis and chemical enhancer (nerolidol) produced no further enhancement for both active agents.
Senyiğit
Taner
T
Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Izmir, Turkey. taner.senyigit@ege.edu.tr
Padula
Cristina
C
Ozer
Ozgen
O
Santi
Patrizia
P
D000287:Administration, Topical; D000305:Adrenal Cortex Hormones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002990:Clobetasol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D053138:Cyclohexenes / Q000494:pharmacology; D004431:Ear, External; D005026:Ethylene Glycols / Q000494:pharmacology; D005782:Gels / Q000138:chemical synthesis / Q000737:chemistry; D007478:Iontophoresis / Q000379:methods; D000077222:Limonene; D000068656:Mometasone Furoate; D010539:Permeability; D014677:Pharmaceutical Vehicles / Q000737:chemistry; D011244:Pregnadienediols / Q000008:administration & dosage / Q000493:pharmacokinetics; D012717:Sesquiterpenes / Q000494:pharmacology; D012867:Skin / Q000737:chemistry / Q000187:drug effects; D012869:Skin Absorption / Q000187:drug effects*; D013552:Swine; D013729:Terpenes / Q000494:pharmacology
D000305:Adrenal Cortex Hormones; D000893:Anti-Inflammatory Agents; D053138:Cyclohexenes; D005026:Ethylene Glycols; D005782:Gels; D014677:Pharmaceutical Vehicles; D011244:Pregnadienediols; D012717:Sesquiterpenes; D013729:Terpenes; D000068656:Mometasone Furoate; D000077222:Limonene; C010111:carbitol; D002990:Clobetasol; C037055:nerolidol