载酮康唑niosome(酮体)用于皮肤念珠菌病药物递送的制备和体外评价

Q4 Pharmacology, Toxicology and Pharmaceutics
K. Morteza-Semnani, M. Saeedi, J. Akbari, M. Moazeni, A. Babaei, R. Negarandeh, M. Azizi, M. Eghbali, S. M. H. Hashemi
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引用次数: 0

摘要

背景:近年来,纳米体在药物传递中越来越受欢迎。本研究旨在探讨酮康唑负载niosome(酮体)的特性、细胞安全性和抗真菌活性。方法:采用超声法制备含胆固醇、非离子表面活性剂和酮康唑的酮体。采用动态光散射(DLS)、差示扫描量热法(DSC)、粉末x射线衍射仪(PXRD)、扫描电镜(SEM)和衰减全反射-傅里叶变换红外(ATR-FTIR)光谱分析了酮体的尺寸特征、形态特征以及酮康唑在酮体中的物理化学性质。并对酮体的溶出率、细胞安全性和抗真菌性能进行了研究。结果:随着胆固醇的增加,酮体的粒径由491.400±10.622 nm减小到121.300±7.274 nm。进一步研究发现,改变胆固醇与表面活性剂的比例可以将zeta电位从-27.866±1.069 mV调节到-12.500±1.153 mV。当酮体中胆固醇浓度较高时,酮康唑的包封率最高,约为87%。胆固醇与表面活性剂比最大的酮体释放速度最快。此外,细胞活力测定显示,酮体与纯药物相比具有更低的细胞毒性。酮体的细胞存活率估计约为90% (HGF细胞系)。在对白色念珠菌进行测试时,酮体的MIC低于纯药物。结论:优化后的载酮康唑niosome可作为酮康唑药物递送的纳米囊泡,为皮肤念珠菌病的治疗开辟了新的途径。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and In-vitro evaluation of ketoconazole-loaded niosome (ketosome) for drug delivery to cutaneous candidiasis
Background: Recently, niosomes are becoming popular in drug delivery. The current work aimed to investigate the characteristics, cellular safety, and antifungal activity of ketoconazole-loaded niosome (ketosome). Methods: Ultrasonic approach was employed to prepare ketosome including cholesterol, nonionic surfactant and ketoconazole. The size characteristics and morphological features of ketosome and physicochemical properties of ketoconazole in ketosomes were evaluated using dynamic light scattering (DLS), differential scanning calorimetry (DSC), powder x-ray diffractometer (PXRD), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy. Also, the dissolution rate, cellular safety test and antimycotic properties of ketosome were examined. Results: According to the results, the particle size of the ketosome decreased from 491.400±10.622 to 121.300±7.274 nm by the increment of cholesterol. According to further research, changes in the cholesterol:surfactants ratio can modulate the zeta potential from -27.866±1.069 to -12.500±1.153 mV. The highest entrapment of ketoconazole was about 87% when the cholesterol concentration in the ketosome was high. Ketosome with the maximum cholesterol:surfactants ratio showed the fastest drug release. Furthermore, the cell viability assay revealed that the ketosome had lower cytotoxicity in comparison with pure drug. The cell viability of the ketosome was estimated to be about 90% (HGF cell line). The ketosome had a lower MIC than the pure drug when tested against Candida albicans. Conclusion: The results of this study revealed that the optimized ketoconazole-loaded niosome could be used as a possible nanovesicle for ketoconazole drug delivery, potentially opening up new ways for the management of cutaneous candidiasis complaints.
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