Preparation and in vitro evaluation of chitosan microgranules with clotrimazole

Acta Pol Pharm. 2012 May-Jun;69(3):509-13.

Abstract

Mucoadhesive polymers have gained much attention due to the possibility to overcome physiological barriers in long-term drug delivery. Chitosan is a biocompatible and non-toxic chitin derivative, which due to its mucoadhesive properties enables to obtain prolonged drug delivery. The aim of this study was to formulate and in vitro evaluate chitosan microgranules with clotrimazole. Microgranules were prepared by the wet-granulation method using pentabasic tripolyphosphate (TPP) as an ion cross-linker. It was shown that crosslinked chitosan significantly prolonged the release of clotrimazole. Microgranules in formulation F4 (with chitosan:clotrimazole:TPP ratio 5:1:1) not only maintained regular surface morphology, but also ensured prolonged release of clotrimazole over the period of 6 h. The obtained results indicate that chitosan is a suitable polymer for developing a sustained-release dosage form of clotrimazole for local delivery.

MeSH terms

  • Adhesiveness
  • Biocompatible Materials / administration & dosage
  • Biocompatible Materials / chemistry
  • Chemistry, Pharmaceutical
  • Chitosan / chemistry*
  • Clotrimazole / administration & dosage*
  • Clotrimazole / chemistry*
  • Delayed-Action Preparations
  • Drug Delivery Systems / methods
  • Microspheres
  • Polyphosphates / chemistry

Substances

  • Biocompatible Materials
  • Delayed-Action Preparations
  • Polyphosphates
  • Chitosan
  • Clotrimazole
  • triphosphoric acid