Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

Abstract

The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous.


Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC

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Author Biographies

Monica RP Rao, Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune 411001, Maharashtra, India

Associate Professor, Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune 411001, Maharashtra, India

Gajanan Paul, Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune 411001, Maharashtra, India

Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune 411001, Maharashtra, India

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Rao M, Paul G. Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis. JDDT [Internet]. 15Nov.2021 [cited 1Dec.2021];11(6):6-4. Available from: https://jddtonline.info/index.php/jddt/article/view/5116