Deoxycholate hydrogels of betamethasone-17-valerate intended for topical use: In vitro and in vivo evaluation

Int J Pharm. 2011 Jan 17;403(1-2):123-9. doi: 10.1016/j.ijpharm.2010.10.036. Epub 2010 Nov 1.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents* / administration & dosage
  • Anti-Inflammatory Agents* / chemistry
  • Anti-Inflammatory Agents* / pharmacokinetics
  • Betamethasone Valerate* / administration & dosage
  • Betamethasone Valerate* / chemistry
  • Betamethasone Valerate* / pharmacokinetics
  • Chromatography, High Pressure Liquid
  • Deoxycholic Acid / chemistry*
  • Disease Models, Animal
  • Drug Carriers / chemistry*
  • Drug Stability
  • Edema / drug therapy
  • Edema / metabolism
  • Hydrogels / chemistry*
  • In Vitro Techniques
  • Male
  • Mechanical Phenomena
  • Rats
  • Rats, Wistar
  • Rheology
  • Skin / metabolism
  • Skin Absorption

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Hydrogels
  • Deoxycholic Acid
  • Betamethasone Valerate