Deoxycholate hydrogels of betamethasone-17-valerate intended for topical use: In vitro and in vivo evaluation.
The aim of this study was to evaluate the suitability of sodium-deoxycholate (Na-DOC) gels containing betamethasone-17-valerate (BMV) for topical application. The gels were characterized for rheological and textural properties. The in vitro flux of BMV from Na-DOC gels across rat skin was 2.5 (0.05% gel) and 8.5 times (0.1% gel) higher compared to the commercial cream (0.1%), respectively. The pharmacodynamic responses after in vivo topical application in rats were also determined. A significant correlation between anti-inflammatory activity and in vitro permeation of BMV was observed. Na-DOC gels produced significantly higher edema inhibition compared to commercial cream at all time intervals. Finally, according to the results of histology studies, Na-DOC gel has no irritant effect on the skin. In conclusion, Na-DOC gel formulation could be suggested as a promising alternative system for the topical application of BMV.
Ege University, Department of Pharmaceutical Technology, 35100 Bornova, Izmir, Turkey. taner.senyigit@ege.edu.tr
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D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001624:Betamethasone Valerate / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D003840:Deoxycholic Acid / Q000737:chemistry*; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004487:Edema / Q000188:drug therapy / Q000378:metabolism; D020100:Hydrogels / Q000737:chemistry*; D066298:In Vitro Techniques; D008297:Male; D055595:Mechanical Phenomena; D051381:Rats; D017208:Rats, Wistar; D012212:Rheology; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D020100:Hydrogels; D003840:Deoxycholic Acid; D001624:Betamethasone Valerate