Meloxicam β-cyclodextrin transdermal gel: physicochemical characterization and in vitro dissolution and diffusion studies

Curr Drug Deliv. 2011 Jul;8(4):381-91. doi: 10.2174/156720111795767942.

Abstract

The aim of the study was to develop a Meloxicam (ME) transdermal gel formulations based on complexation with β-cyclodextrin. ME β-Cyclodextrin gel formulations were prepared using four different gel bases with different concentrations and different permeation enhancers. The developed formulations were examined for their in vitro characteristics and their diffusion through a mouse skin. The gel formulations were prepared successfully. Physicochemical characterization of ME β-CD complex in solution state by phase solubility revealed 1:1 M complexation of ME with β-Cyclodextrin. ME release profiles from the inclusion complex were superior over ME alone. Hydroxypropyl methyl cellulose 15% w/w gel base was proven to be a suitable base for ME inclusion complex formulation as it provides a high drug release than other studied bases. ME β-CD complex gel formulations containing oleic acid (1% w/w) or (5% w/w) cineol used as permeation enhancers in (15% w/w) HPMC gel base were proven to provide a higher diffusion rate of the drug through the mouse skin. This is very promising in providing analgesic activity of meloxicam via topical route of administration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Diffusion
  • Dosage Forms
  • Gels / administration & dosage
  • Gels / chemical synthesis
  • Gels / chemistry*
  • Male
  • Meloxicam
  • Mice
  • Permeability
  • Skin / drug effects
  • Skin / metabolism
  • Solubility
  • Spectroscopy, Fourier Transform Infrared / methods
  • Thiazines / administration & dosage
  • Thiazines / chemistry*
  • Thiazoles / administration & dosage
  • Thiazoles / chemistry*
  • beta-Cyclodextrins / administration & dosage
  • beta-Cyclodextrins / chemistry*

Substances

  • Dosage Forms
  • Gels
  • Thiazines
  • Thiazoles
  • beta-Cyclodextrins
  • Meloxicam