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载18-β-甘草次酸的聚乳酸-羟基乙酸共聚物纳米粒的制备及抗菌活性评价

Preparation and Antibacterial Activity Evaluation of 18-β-glycyrrhetinic Acid Loaded PLGA Nanoparticles.

作者信息

Darvishi Behrad, Manoochehri Saeed, Kamalinia Golnaz, Samadi Nasrin, Amini Mohsen, Mostafavi Seyyed Hossein, Maghazei Shahab, Atyabi Fatemeh, Dinarvand Rassoul

机构信息

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

Drug and Food Control Department, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2015 Spring;14(2):373-83.

Abstract

The aim of the present study was to formulate poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with 18-β-glycyrrhetinic acid (GLA) with appropriate physicochemical properties and antimicrobial activity. GLA loaded PLGA nanoparticles were prepared with different drug to polymer ratios, acetone contents and sonication times and the antibacterial activity of the developed nanoparticles was examined against different gram-negative and gram-positive bacteria. The antibacterial effect was studied using serial dilution technique to determine the minimum inhibitory concentration of nanoparticles. Results demonstrated that physicochemical properties of nanoparticles were affected by the above mentioned parameters where nanoscale size particles ranging from 175 to 212 nm were achieved. The highest encapsulation efficiency (53.2 ± 2.4%) was obtained when the ratio of drug to polymer was 1:4. Zeta potential of the developed nanoparticles was fairly negative (-11±1.5). In-vitro release profile of nanoparticles showed two phases: an initial phase of burst release for 10 h followed by a slow release pattern up to the end. The antimicrobial results revealed that the nanoparticles were more effective than pure GLA against P. aeuroginosa, S. aureus and S. epidermidis. This improvement in antibacterial activity of GLA loaded nanoparticles when compared to pure GLA may be related to higher nanoparticles penetration into infected cells and a higher amount of GLA delivery in its site of action. Herein, it was shown that GLA loaded PLGA nanoparticles displayed appropriate physicochemical properties as well as an improved antimicrobial effect.

摘要

本研究的目的是制备负载18-β-甘草次酸(GLA)的聚乳酸-羟基乙酸共聚物(PLGA)纳米颗粒,使其具有合适的物理化学性质和抗菌活性。采用不同的药物与聚合物比例、丙酮含量和超声处理时间制备了负载GLA的PLGA纳米颗粒,并检测了所制备纳米颗粒对不同革兰氏阴性菌和革兰氏阳性菌的抗菌活性。采用系列稀释技术研究抗菌效果,以确定纳米颗粒的最低抑菌浓度。结果表明,上述参数会影响纳米颗粒的物理化学性质,所制备的纳米颗粒粒径范围为175至212 nm。当药物与聚合物比例为1:4时,获得了最高的包封率(53.2±2.4%)。所制备纳米颗粒的zeta电位呈相当负的值(-11±1.5)。纳米颗粒的体外释放曲线呈现两个阶段:初始阶段为10小时的突释,随后是直至结束的缓释模式。抗菌结果显示,纳米颗粒对铜绿假单胞菌、金黄色葡萄球菌和表皮葡萄球菌的抗菌效果比纯GLA更有效。与纯GLA相比,负载GLA的纳米颗粒抗菌活性的提高可能与纳米颗粒更高地渗透到感染细胞中以及在其作用部位递送更高量的GLA有关。在此表明,负载GLA的PLGA纳米颗粒具有合适的物理化学性质以及改善的抗菌效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5e/4403053/3617cc1170b0/ijpr-14-373-g001.jpg

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