期刊
MOLECULES
卷 27, 期 14, 页码 -出版社
MDPI
DOI: 10.3390/molecules27144425
关键词
antimycotic activity; dissolution rate; fluconazole; inclusion complexation; phase solubility; sulfonatocalix[4]naphthalene
资金
- Deanship of Scientific Research-Mutah University [2020/358]
This study assessed the interaction between fluconazole and sulfonatocalix[4]naphthalene, finding that they formed a stable inclusion complex which significantly enhanced dissolution performance and antimycotic activity.
The study aims to assess the interaction between fluconazole and sulfonatocalix[4]naphthalene towards enhancing its dissolution performance and antimycotic activity. A solubility study was carried out at different pH conditions, and the results revealed the formation of a 1:1 molar ratio fluconazole-sulfonatocalix[4]naphthalene inclusion complex with an A(L) type phase solubility diagrams. The solid powder systems of fluconazole-sulfonatocalix[4]naphthalene were prepared using kneaded and co-evaporation techniques and physical mixtures. DCS, PXRD, TGA-DTG, FT-IR, and in vitro dissolution performance characterize the prepared systems. According to physicochemical characterization, the co-evaporation approach produces an amorphous inclusion complex of the drug inside the cavity of sulfonatocalix[4]naphthalene. The co-evaporate product significantly increased the drug dissolution rate up to 93 +/- 1.77% within 10 min, unlike other prepared solid powders. The antimycotic activity showed an increase substantially (p <= 0.05, t-test) antimycotic activity of fluconazole co-evaporate mixture with sulfonatocalix[4]naphthalene compared with fluconazole alone against clinical strains of Candida albicans and Candida glabrata. In conclusion, sulfonatocalix[4]naphthalene could be considered an efficient complexing agent for fluconazole to enhance its aqueous solubility, dissolution performance, and antimycotic activity.
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