Ciprofloxacin-encapsulated poly(DL-lactide-co-glycolide) nanoparticles and its antibacterial activity
Ciprofloxacin-encapsulated poly(DL-lactide-co-glycolide) nanoparticles and its antibacterial activity
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DOI：
10.1016/j.ijpharm.2007.11.001
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发表时间：
2008-03-20
影响因子：
5.8
通讯作者：
Nah, Jae-Woon
中科院分区：
文献类型：
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作者：
Jeong, Young-Il;Na, Hee-Sam;Nah, Jae-Woon
本研究的目的是制备环丙沙星HCl （CIP）包封聚乳酸-羟基乙酸酯（PLGA）共聚物纳米颗粒，并对病原菌大肠杆菌（E. coli）进行体外和体内抑菌活性评价。采用多乳液溶剂蒸发法制备了cip包封的PLGA纳米颗粒。PLGA纳米颗粒呈球形，粒径在100 ~ 300 nm之间。由于CIP的水溶性，负载效率低于50% （w/w）。在药物释放研究中，CIP表现出12 h的初始爆发效应，然后连续释放2周。体外抗菌活性测试表明，CIP包封的纳米颗粒由于其缓释特性，抗菌活性较游离CIP低。然而，CIP包封的PLGA纳米颗粒（剂量：25 mg CIP/kg小鼠）由于纳米颗粒的缓释特性，可以有效抑制细菌的生长，而游离CIP对细菌生长的抑制效果较差。这些结果表明，cip包封的PLGA纳米颗粒在体内具有良好的抑制细菌生长的效果。(C) 2007 Elsevier B.V.版权所有
The aim of this study was to prepare ciprofloxacin HCl (CIP)-encapsulated poly(DL-lactide-co-glycolide) (PLGA) copolymer nanoparticles and its antibacterial potential was evaluated with pathogenic bacteria, Escherichia coli (E. coli), in vitro and in vivo. CIP-encapsulated nanoparticles of PLGA were prepared by multiple emulsion solvent evaporation method. PLGA nanoparticles showed spherical shapes with particle sizes around 100-300 nm. Loading efficiency was lower than 50% (w/w) because of water-solubility properties of CIP. At drug release study, CIP showed initial burst effect for 12 h and then continuously released for 2 weeks. At in vitro antibacterial activity test, CIP-encapsulated nanoparticles showed relatively lower antibacterial activity compared to free CIP due to the sustained release characteristics of nanoparticles. However, CIP-encapsulated PLGA nanoparticles (doses: 25 mg CIP/kg of mice) effectively inhibited the growth of bacteria due to the sustained release characteristics of nanoparticles, while free CIP was less effective on the inhibition of bacterial growth. These results indicated that CIP-encapsulated PLGA nanoparticles have superior effectiveness to inhibit the growth of bacteria in vivo. (C) 2007 Elsevier B.V. All rights reserved.