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负载利福平的介孔二氧化硅纳米颗粒的制备及其表征:一种潜在的肺部给药系统

Preparation and characterization of rifampin loaded mesoporous silica nanoparticles as a potential system for pulmonary drug delivery.

作者信息

Mohseni Meysam, Gilani Kambiz, Mortazavi Seyed Alireza

机构信息

Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2015 Winter;14(1):27-34.

Abstract

The goal of this research is to determine the feasibility of loading rifampin into mesoporous silica nanoparticles. Rifampin was selected as a model lipophilic molecule since it is a well-documented and much used anti tuberculosis drug. The mesoporous silica nanoparticles were prepared by using tetraethyl ortho silicate and cetyltrimethyl ammonium bromide (as surfactant). The prepared nanoparticles were characterized in terms of their particle size measurement and porosimetry. The results showed that the particle size is 218 ± 46 nm (mean ± SD) and surface area is 816 m(2)g(-1). In order to load rifampin within the mesopores, adsorption experiments using three different solvents (methanol, water and dimethyl sulfoxide) were carried out. The loading procedure resulted in a significant improvement in the amount of rifampin loaded into mesoporous silica nanoparticles and methanol was found to be a suitable solvent, providing a drug entrapment efficiency of 52 %. Rifampin loaded nanoparticles underwent different in-vitro tests including, SEM and drug release. The in-vitro drug release was investigated using buffer phosphate (pH=7.4). Regarding the drug release study, a biphasic pattern of release was observed. The drug-loaded mesoporous silica nanoparticles were capable of releasing 95% of their drug content after 24 h, following a faster release in the first four hours. The prepared rifampin loaded nanoparticles seem to have potential for use as a pulmonary drug delivery.

摘要

本研究的目的是确定将利福平载入介孔二氧化硅纳米颗粒的可行性。利福平作为一种记录完备且广泛使用的抗结核药物,被选作亲脂性分子模型。采用正硅酸乙酯和十六烷基三甲基溴化铵(作为表面活性剂)制备介孔二氧化硅纳米颗粒。通过粒度测量和孔隙率测定对制备的纳米颗粒进行表征。结果表明,粒径为218±46nm(平均值±标准差),表面积为816m²/g。为了将利福平载入介孔内,使用三种不同溶剂(甲醇、水和二甲基亚砜)进行吸附实验。载入过程使载入介孔二氧化硅纳米颗粒的利福平量有显著提高,且发现甲醇是一种合适的溶剂,药物包封率为52%。载入利福平的纳米颗粒进行了包括扫描电子显微镜和药物释放在内的不同体外测试。使用磷酸盐缓冲液(pH = 7.4)研究体外药物释放。关于药物释放研究,观察到双相释放模式。载药介孔二氧化硅纳米颗粒在前4小时快速释放后,24小时内能够释放其95%的药物含量。制备的载有利福平的纳米颗粒似乎有作为肺部药物递送的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e87/4277616/bb5155e168da/ijpr-14-027-g001.jpg

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