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载克拉霉素的聚乳酸-羟基乙酸共聚物纳米粒对幽门螺杆菌临床菌株的抗菌作用研究

Study of Antimicrobial Effects of Clarithromycin Loaded PLGA Nanoparticles against Clinical Strains of Helicobacter pylori.

作者信息

Lotfipour F, Valizadeh H, Milani M, Bahrami N, Ghotaslou R

机构信息

Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.

School of Advanced Medicine, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Drug Res (Stuttg). 2016 Jan;66(1):41-5. doi: 10.1055/s-0035-1548910. Epub 2015 Apr 28.

Abstract

Clarithromycin (CLR) formulation was prepared as PLGA nanoparticles in order to enhance the therapeutic effects using the distinctive features of a nanoparticulate delivery system. CLR loaded PLGA nanoparticles were prepared by Quasi Emulsion Solvent Diffusion (QESD) method using Poly lactic-co-Glycolic Acid (PLGA) as a biodegradable polymer. Antibacterial activity of the prepared formulations was evaluated against clinical strains of Helicobacter pylori, isolated from gastric biopsies of patients with gastritis, duodenal ulcer, peptic ulcer, and gastroesophageal reflux disease undergoing endoscopy, by using agar dilution method.Spherical nanoparticles with relatively narrow size distribution (between 200 and 800 nm) in the size range of 305 ± 138, 344 ± 148 and 362 ± 110 nm were achieved for F22, F23 and F23 respectively. CLR encapsulation percentages were measured to be 57.4 ± 4.3 to 80.2 ± 4.0%. CLR loaded PLGA nanoparticles showed equal or enhanced eradication effect against H. pylori strains according to the declined MIC values in comparison with the untreated CLR.In conclusion, the prepared CLR nanoformulation showed appropriate physicochemical properties and improved activity against H. pylori that could be a suitable candidate for oral preparations.

摘要

为利用纳米颗粒递送系统的独特特性增强治疗效果,制备了克拉霉素(CLR)制剂,制成聚乳酸-乙醇酸共聚物(PLGA)纳米颗粒。以聚乳酸-乙醇酸共聚物(PLGA)作为可生物降解聚合物,通过准乳液溶剂扩散(QESD)法制备了载有CLR的PLGA纳米颗粒。采用琼脂稀释法,对从接受内镜检查的胃炎、十二指肠溃疡、消化性溃疡和胃食管反流病患者的胃活检标本中分离出的幽门螺杆菌临床菌株,评估所制备制剂的抗菌活性。F22、F23和F23分别获得了尺寸范围在305±138、344±148和362±110nm之间、尺寸分布相对较窄(200至800nm)的球形纳米颗粒。测得CLR包封率为57.4±4.3%至80.2±4.0%。与未处理的CLR相比,载有CLR的PLGA纳米颗粒根据MIC值的下降显示出对幽门螺杆菌菌株同等或增强的根除效果。总之,所制备的CLR纳米制剂显示出合适的理化性质以及对幽门螺杆菌的活性增强,可能是口服制剂的合适候选物。

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