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黏菌素甲磺酸钠脂质纳米粒的稳定性研究

Stability study of sodium colistimethate-loaded lipid nanoparticles.

作者信息

Moreno-Sastre M, Pastor M, Esquisabel A, Sans E, Viñas M, Bachiller D, Pedraz J L

机构信息

a NanoBioCel Group, Laboratory of Pharmaceutics , School of Pharmacy, University of the Basque Country (UPV/EHU) , Vitoria-Gasteiz , Spain.

b Biomedical Research Networking Centre in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Vitoria-Gasteiz , Spain.

出版信息

J Microencapsul. 2016 Nov;33(7):636-645. doi: 10.1080/02652048.2016.1242665. Epub 2016 Oct 14.

Abstract

In the last decades, the encapsulation of antibiotics into nanoparticulate carriers has gained increasing attention for the treatment of infectious diseases. Sodium colistimethate-loaded solid lipid nanoparticles (Colist-SLNs) and nanostructured lipid carriers (Colist-NLCs) were designed aiming to treat the pulmonary infection associated to cystic fibrosis patients. The nanoparticles were freeze-dried using trehalose as cryoprotectant. The stability of both nanoparticles was analysed over one year according to the International Conference of Harmonisation (ICH) guidelines by determining the minimum inhibitory concentration (MIC) against clinically isolated Pseudomonas aeruginosa strains and by studying their physico-chemical characteristics. The results showed that Colist-SLNs lost their antimicrobial activity at the third month; on the contrary, the antibacterial activity of Colist-NLCs was maintained throughout the study within an adequate range (MIC ≤16 μg/mL). In addition, Colist-NLCs exhibited suitable physico-chemical properties at 5 °C and 25 °C/60% relative humidity over one year. Altogether, Colist-NLCs proved to have better stability than Colist-SLNs.

摘要

在过去几十年中,将抗生素封装到纳米颗粒载体中用于治疗传染病已越来越受到关注。设计了负载多粘菌素甲磺酸钠的固体脂质纳米粒(Colist-SLNs)和纳米结构脂质载体(Colist-NLCs),旨在治疗与囊性纤维化患者相关的肺部感染。使用海藻糖作为冷冻保护剂对纳米颗粒进行冻干。根据国际协调会议(ICH)指南,通过测定对临床分离的铜绿假单胞菌菌株的最低抑菌浓度(MIC)并研究其物理化学特性,对两种纳米颗粒的稳定性进行了为期一年的分析。结果表明,Colist-SLNs在第三个月失去了抗菌活性;相反,Colist-NLCs的抗菌活性在整个研究过程中保持在适当范围内(MIC≤16μg/mL)。此外,Colist-NLCs在一年中5°C和25°C/60%相对湿度条件下表现出合适的物理化学性质。总体而言,Colist-NLCs被证明比Colist-SLNs具有更好的稳定性。

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