Itraconazole-Loaded Ufasomes: Evaluation, Characterization, and Anti-Fungal Activity against Candida albicans

被引:5
|
作者
Hashem, Sara M. M. [1 ]
Gad, Mary K. K. [1 ]
Anwar, Hend M. M. [2 ]
Saleh, Neveen M. M. [3 ]
Shamma, Rehab N. N. [4 ]
Elsherif, Noha I. I. [5 ]
机构
[1] Natl Org Drug Control & Res, Cairo 12622, Egypt
[2] Egyptian Drug Author, Dept Biochem, Cairo 12611, Egypt
[3] Egyptian Drug Author, Dept Microbiol, Cairo 12611, Egypt
[4] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11562, Egypt
[5] Heliopolis Univ, Fac Pharm, Dept Pharmaceut & Pharmaceut Technol, Cairo 11785, Egypt
关键词
itraconazole; ufasomes; oleic acid; Candida albicans; microbiology; TOLL-LIKE RECEPTORS; IN-VITRO; ACID VESICLES; RECOGNITION; INFECTIONS; ENHANCEMENT; FLUCONAZOLE; LIPOSOMES; PATHOGENS; DELIVERY;
D O I
10.3390/pharmaceutics15010026
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Numerous obstacles challenge the treatment of fungal infections, including the uprising resistance and the low penetration of available drugs. One of the main active agents against fungal infections is itraconazole (ITZ), with activity against a broad spectrum of fungi while having few side effects. The aim of this study was to design ufasomes, oleic acid-based colloidal carriers, that could encapsulate ITZ to improve its penetration power. Employing a 2(2)3(1) factorial design, the effect of three independent factors (oleic acid amount, cholesterol concentration, and ITZ amount) was investigated and evaluated for the percentage encapsulation efficiency (%EE), particle size (PS), and zeta potential (ZP). Optimization was performed using Design((R)) expert software and the optimized ITZ-loaded ufasomes obtained had %EE of 99.4 +/- 0.7%, PS of 190 +/- 1 nm, and ZP of -81.6 +/- 0.4 mV, with spherical unilamellar morphology and no aggregation. An in vitro microbiological study was conducted to identify the minimum inhibitory concentration of the selected formula against Candida albicans, which was found to be 0.0625 mu g/mL. Moreover, the optimized formula reduced the expression of toll-like receptors-4 and pro-inflammatory cytokine IL-1 beta secretion in the C. albicans-infected fibroblasts, indicating that the proposed ITZ-loaded ufasomes are a promising drug delivery system for ITZ.
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页数:20
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