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载姜黄素聚乳酸-羟基乙酸共聚物油核纳米囊提高溶解度和抗菌活性。

Enhanced curcumin solubility and antibacterial activity by encapsulation in PLGA oily core nanocapsules.

机构信息

School of Life Science, Jiangsu Normal University, Xuzhou 221116, Jiangsu, China.

出版信息

Food Funct. 2020 Jan 29;11(1):448-455. doi: 10.1039/c9fo00901a.

Abstract

Infections caused by bacteria represent an emerging public health threat due to the development of antibiotic resistance in bacteria. Curcumin (CUR), a naturally derived substance, is found to be effective against several bacteria. However, its use is limited by its low water solubility and rapid degradation profile. Polymeric nanocapsules (NCs) represent an interesting drug delivery system with high incorporation rates due to their liquid core. The present study aimed to develop poly-(lactic-co-glycolic acid) (PLGA) NCs for the delivery of CUR for enhancing its solubility and antibacterial activity. The particle size, polydispersity index (PDI), zeta potential and drug entrapment efficiency of CUR NCs with optimal formulation were 158 nm, 0.156, -29.1 mV and 92.64%, respectively. The water solubility of CUR in NCs increased about 1500 fold compared to that of free CUR. TEM and AFM images proved the core-shell structure of PLGA NCs with narrow size distributions. The in vitro release profile of CUR from PLGA NCs showed a burst release in the initial 24 h followed by a sustained release of the interior CUR over 10 days. In vitro antibacterial experiments demonstrate that the minimum inhibitory concentrations (MICs) of CUR NCs were lower than those of free CUR for all different bacterial strains, especially for Gram-negative bacteria. CUR NCs exhibited broad-spectrum antibacterial effects compared with free CUR. These data suggest that these CUR-loaded PLGA NCs may provide a promising strategy as novel antibacterial agents.

摘要

由于细菌对抗生素的耐药性不断发展,由细菌引起的感染已成为一个新出现的公共卫生威胁。姜黄素(CUR)是一种天然存在的物质,已被证明对多种细菌有效。然而,由于其水溶性低和快速降解的特性,其应用受到限制。聚合物纳米胶囊(NCs)因其具有液态核而具有高包封率,是一种很有前途的药物传递系统。本研究旨在开发用于递送 CUR 的聚(乳酸-共-乙醇酸)(PLGA)NCs,以提高其溶解度和抗菌活性。最佳配方的 CUR NCs 的粒径、多分散指数(PDI)、Zeta 电位和药物包封效率分别为 158nm、0.156、-29.1mV 和 92.64%。与游离 CUR 相比,CUR 在 NCs 中的水溶性提高了约 1500 倍。TEM 和 AFM 图像证明了 PLGA NCs 的核壳结构,具有较窄的粒径分布。CUR 从 PLGA NCs 的体外释放曲线显示出在最初 24 小时内的突释,随后在 10 天内持续释放内部 CUR。体外抗菌实验表明,CUR NCs 的最低抑菌浓度(MICs)低于游离 CUR 对所有不同细菌株的 MICs,尤其是对革兰氏阴性菌。CUR NCs 与游离 CUR 相比表现出广谱的抗菌作用。这些数据表明,这些负载 CUR 的 PLGA NCs 可能为新型抗菌剂提供一种有前途的策略。

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