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使用具有天然抗真菌活性的辅料优化载两性霉素B纳米乳剂的局部给药新视角:一项机制与组织病理学研究。

New perspectives in the topical delivery of optimized amphotericin B loaded nanoemulsions using excipients with innate anti-fungal activities: A mechanistic and histopathological investigation.

作者信息

Hussain Afzal, Singh Sima, Webster Thomas J, Ahmad Farhan Jalees

机构信息

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India; Faculty of Pharmacy, S. Sinha College, Aurangabad, Bihar, India.

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.

出版信息

Nanomedicine. 2017 Apr;13(3):1117-1126. doi: 10.1016/j.nano.2016.12.002. Epub 2016 Dec 20.

DOI:10.1016/j.nano.2016.12.002
PMID:28007632
Abstract

This study aimed to develop nanoemulsions (NEs) for the topical delivery of Amphotericin B using lipids and surfactants with innate antifungal activity. NEs were formulated by a slow spontaneous titration method and characterized for particle size, polydispersity index, zeta potential, zone of inhibition (ZOI), in vitro release, enhanced ex vivo rat skin permeation-deposition, hemolysis followed by interaction with the skin using scanning electron microscopy, and histopathology. The ZOI values of the optimized NEs (ANE3) were 21.8±1.5 and 19.7±1.2 mm against A. fumigatus and C. albicans, respectively. The explored excipients and optimized ANE3 elicited hemo-biocompatibility. ANE3 exhibited in vitro sustained release and an enhanced flux value (21.62±1.6 μg/cm/h) as compared to the drug solution and Fungisome without displaying toxicity. Conclusively, ANE3 could be a promising therapeutic approach with enhanced efficacy and safety for treating a wide range of fungal infections topically.

摘要

本研究旨在利用具有固有抗真菌活性的脂质和表面活性剂开发用于两性霉素B局部给药的纳米乳剂(NEs)。通过缓慢自发滴定法制备纳米乳剂,并对其粒径、多分散指数、zeta电位、抑菌圈(ZOI)、体外释放、增强的大鼠皮肤离体渗透沉积、溶血情况进行表征,随后使用扫描电子显微镜和组织病理学研究其与皮肤的相互作用。优化后的纳米乳剂(ANE3)对烟曲霉和白色念珠菌的抑菌圈值分别为21.8±1.5和19.7±1.2毫米。所探索的辅料和优化后的ANE3具有血液生物相容性。与药物溶液和两性霉素B脂质体相比,ANE3表现出体外缓释和更高的通量值(21.62±1.6μg/cm/h),且未显示出毒性。总之,ANE3可能是一种有前景的治疗方法,具有更高的疗效和安全性,可用于局部治疗多种真菌感染。

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