Prolonged antifungal effects of clotrimazole-containing mucoadhesive thermosensitive gels on vaginitis

Jung Yun Chang, Yu Kyoung Oh, Hak Soo Kong, Eun Jung Kim, Dong Deuk Jang, KiTaek Nam, Chong Kook Kim

Research output: Contribution to journalArticle

131 Citations (Scopus)

Abstract

To develop more effective treatment for vaginal candidasis, clotrimazole (CT) was formulated in mucoadhesive thermosensitive gels (MTG). Several MTG formulations composed of poloxamers (P) 407, 188, and polycarbophil (PC) were prepared. P188 and PC increased the mucoadhesiveness but reduced the syringebility of liquid forms of the gels. Based on the balance between the mucoadhesiveness and syringebility, MTG composed of P407/P188/PC (15/15/0.2 or 15/20/0.2) were further studied. Of the two MTG, the formulation with 15% of P188 gelled at higher temperature and revealed lower elastic modulus. In vitro, sustained release of CT from MTG was observed. In vivo antifungal activity of CT, tested against Candida albicans vaginitis in female rats, was significantly prolonged after vaginal delivery using MTG. At 10 days post-dose, the c.f.u. of C. albicans was more than 104-fold decreased in MTG-treated groups. Moreover, the vaginal delivery of CT in MTG enhanced the viability of epithelial cells without affecting the morphology of vaginal mucosa. These results indicate that CT-containing vaginal MTG might be further developed for safe, convenient, and effective treatment of vaginal candidasis with reduced dosing interval.

Original languageEnglish
Pages (from-to)39-50
Number of pages12
JournalJournal of Controlled Release
Volume82
Issue number1
DOIs
Publication statusPublished - 2002 Jul 18

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Clotrimazole
Vaginitis
Gels
Candida albicans
Poloxamer
Elastic Modulus
Mucous Membrane
Epithelial Cells

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Yun Chang, Jung ; Oh, Yu Kyoung ; Soo Kong, Hak ; Jung Kim, Eun ; Deuk Jang, Dong ; Nam, KiTaek ; Kim, Chong Kook. / Prolonged antifungal effects of clotrimazole-containing mucoadhesive thermosensitive gels on vaginitis. In: Journal of Controlled Release. 2002 ; Vol. 82, No. 1. pp. 39-50.
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abstract = "To develop more effective treatment for vaginal candidasis, clotrimazole (CT) was formulated in mucoadhesive thermosensitive gels (MTG). Several MTG formulations composed of poloxamers (P) 407, 188, and polycarbophil (PC) were prepared. P188 and PC increased the mucoadhesiveness but reduced the syringebility of liquid forms of the gels. Based on the balance between the mucoadhesiveness and syringebility, MTG composed of P407/P188/PC (15/15/0.2 or 15/20/0.2) were further studied. Of the two MTG, the formulation with 15{\%} of P188 gelled at higher temperature and revealed lower elastic modulus. In vitro, sustained release of CT from MTG was observed. In vivo antifungal activity of CT, tested against Candida albicans vaginitis in female rats, was significantly prolonged after vaginal delivery using MTG. At 10 days post-dose, the c.f.u. of C. albicans was more than 104-fold decreased in MTG-treated groups. Moreover, the vaginal delivery of CT in MTG enhanced the viability of epithelial cells without affecting the morphology of vaginal mucosa. These results indicate that CT-containing vaginal MTG might be further developed for safe, convenient, and effective treatment of vaginal candidasis with reduced dosing interval.",
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Prolonged antifungal effects of clotrimazole-containing mucoadhesive thermosensitive gels on vaginitis. / Yun Chang, Jung; Oh, Yu Kyoung; Soo Kong, Hak; Jung Kim, Eun; Deuk Jang, Dong; Nam, KiTaek; Kim, Chong Kook.

In: Journal of Controlled Release, Vol. 82, No. 1, 18.07.2002, p. 39-50.

Research output: Contribution to journalArticle

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