期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 111, 期 2, 页码 458-468出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2021.09.019
关键词
Terconazole; Eudragit RLPO (R); Cationic nanoparticles; Mucoadhesive; Antimycotic activity; Candida albicans
Terconazole is an antifungal drug with poor water solubility, limiting its ocular absorption. This study aimed to enhance its antimycotic activity in the eyes by developing terconazole-loaded polymeric nanoparticles, and the characteristics and drug release performance of the nanoparticles were evaluated.
Terconazole (TCZ) is a broad-spectrum antifungal triazole that is particularly active against Candida species, but its poor water solubility hinders its ocular absorption and restricts its application. This study aims to fabricate TCZ-loaded cationic polymeric nanoparticles to enhance the ocular delivery and antimycotic activity of terconazole. TCZ-loaded nanoparticles were developed by nanoprecipitation method employing Eudragit RLPO (R). They were characterized by entrapment efficiency (EE%), particle size (PS), zeta potential (ZP), morphology, Fourier transform infrared spectroscopy (FT-IR), and X-ray powder diffraction (XRPD). In-vitro antimycotic activity was evaluated by measuring zone of inhibition (ZI), minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). The developed nanoparticles were spherical with moderate to high EE% (44.03-71.14%), a nanometric PS (49.41-78.72 nm), and a positively charged ZP (>= +21.47). In-vitro release studies revealed sustained release of drug up to 24 h. FT-IR of TCZ-loaded nanoparticles revealed distinctive peaks for Eudragit RLPO (R) and Poloxamer-188, with disappearance of the TCZ characteristic peaks. XRPD revealed the amorphous state of TCZ within the polymer matrix. Mucoadhesive studies proved the mucoadhesive property of the developed TCZ nanoparticles. In-vitro antimycotic studies, assessed by ZI, MIC and MFC, revealed enhanced antimycotic activity of TCZ-loaded nanoparticles against Candida albicans, relative to plain TCZ. No irritation or abnormal changes to the rabbits' eyes for plain and medicated polymeric nanoparticles were found by the in-vivo Draize test. These findings reveal that the cationic polymeric nanoparticles can be regarded as a potential drug delivery system for enhancing the ocular antimycotic activity of TCZ. (C) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
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