期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 174, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ejps.2022.106204
关键词
Chitosan; Alginate; Clotrimazole; Polyelectrolyte foam; Drug release; Antifungal activity
资金
- University of Copenhagen, Denmark and Oversea Study Program of Guangzhou Elite Project for Jianfei Huang [JY201622]
This study investigated the effect of graphene oxide (GO) and the composition of excipients on the release and antifungal activities of clotrimazole-loaded buccal foams. The results showed that the addition of GO increased the mechanical strength of the foams and accelerated the release of clotrimazole. However, it did not significantly affect the antifungal activity of clotrimazole-loaded foams.
Polyelectrolyte complexes (PECs) have been used as the matrix of solid foams for drug delivery. This study aimed at investigating the effect of graphene oxide (GO) and the composition of excipients in chitosan/alginate-based buccal foams on the clotrimazole release and antifungal activities. The investigation has been focused on the interactions of the drug with excipients in the foams, and the changes of ionization degree upon exposure to various media are discussed. The solid foams were prepared by mixing the excipients and clotrimazole via probe sonication, followed by a freeze-drying method. The pH values of the formulations were measured during the foam preparation process to estimate the ionization degree of clotrimazole and the other excipients. The foam matrix was the PECs between the cationic chitosan and anionic alginate. The mechanical strength of clotrimazole-loaded foams was lower than that of drug-free foams due to the positively charged clotrimazole interacting with the anionic alginate and interfering the PECs between chitosan and alginate. Addition of GO in the clotrimazole-loaded matrix made the foams mechanically stronger and contributed to a faster release of clotrimazole from the buccal foams by disrupting the electrostatic interactions between alginate and clotrimazole. However, addition of 1 wt% GO in the formulations didn't affect the antifungal activity of clotrimazoleloaded foams significantly. A lower amount GO in the formulation may be required for enhancing the anti fungal effect, which should be further investigated in future.
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