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通过甘露糖化多壁碳纳米管靶向巨噬细胞的两性霉素 B

Macrophages targeting of amphotericin B through mannosylated multiwalled carbon nanotubes.

机构信息

Department of Pharmaceutical Sciences, Pharmaceutics Research Laboratory, Dr. H. S. Gour University, Sagar, Madhya Pradesh, India.

出版信息

J Drug Target. 2012 Aug;20(7):593-604. doi: 10.3109/1061186X.2012.697168. Epub 2012 Jun 12.

DOI:10.3109/1061186X.2012.697168
PMID:22690657
Abstract

The objective of the present investigation was to assess the potential of polysaccharide (mannose) conjugated engineered multiwalled carbon nanotubes (MWCNTs) bearing Amphotericin B (AmB) formulation for site-specific delivery to macrophages. The mannosylated carbon nanotubes (CNTs) were synthesized and AmB was efficiently loaded using dialysis diffusion method. The synthesized mannosylated MWCNTs were characterized by various physicochemical and physiological parameters such as fourier transform infrared (FTIR) spectroscopy, scanning and transmission electron microscopy (SEM & TEM), drug loading and entrapment efficiency, in-vitro release kinetics, in-vivo study and toxicological investigation. AmB loaded mannosylated MWCNTs (AmBitubes) was found to be nanometric in size (500 nm) with tubular structure and good entrapment efficiency (75.46 ± 1.40%). In-vitro AmB from AmBitubes was found to be released in a controlled manner at pH 4, 7.4 and 10, with enhanced cell uptake and higher disposition in macrophage-rich organs, thereby indicating the site-specific drug delivery. The results suggest that AmBitubes could be employed as efficient nano-carrier for antileishmanial therapy.

摘要

本研究旨在评估多糖(甘露糖)偶联载两性霉素 B(AmB)的工程化多壁碳纳米管(MWCNTs)在巨噬细胞靶向递送上的潜力。通过透析扩散法,成功地将 AmB 负载到合成的甘露糖化 MWCNTs 上。通过傅里叶变换红外(FTIR)光谱、扫描和透射电子显微镜(SEM 和 TEM)、药物负载和包封效率、体外释放动力学、体内研究和毒理学研究等多种物理化学和生理参数对合成的甘露糖化 MWCNTs 进行了表征。负载 AmB 的甘露糖化 MWCNTs(AmBitubes)的粒径为纳米级(500nm),呈管状结构,包封效率良好(75.46±1.40%)。在体外,AmBitubes 中的 AmB 在 pH 4、7.4 和 10 下以可控的方式释放,细胞摄取增强,在富含巨噬细胞的器官中分布更高,表明具有靶向药物递送的作用。结果表明,AmBitubes 可作为有效的抗利什曼原虫治疗的纳米载体。

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