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壳聚糖修饰的具有多功能表面的 PLGA 纳米粒用于改善药物传递。

Chitosan-modified PLGA nanoparticles with versatile surface for improved drug delivery.

机构信息

Institute for Frontier Materials, Deakin University, Waurn Ponds, VIC 3216, Australia.

出版信息

AAPS PharmSciTech. 2013 Jun;14(2):585-92. doi: 10.1208/s12249-013-9943-3. Epub 2013 Mar 6.

Abstract

Shortage of functional groups on surface of poly(lactide-co-glycolide) (PLGA)-based drug delivery carriers always hampers its wide applications such as passive targeting and conjugation with targeting molecules. In this research, PLGA nanoparticles were modified with chitosan through physical adsorption and chemical binding methods. The surface charges were regulated by altering pH value in chitosan solutions. After the introduction of chitosan, zeta potential of the PLGA nanoparticle surface changed from negative charge to positive one, making the drug carriers more affinity to cancer cells. Functional groups were compared between PLGA nanoparticles and chitosan-modified PLGA nanoparticles. Amine groups were exhibited on PLGA nanoparticle surface after the chitosan modification as confirmed by Fourier transform infrared spectroscopy and X-ray photoelectron spectroscopy. The modified nanoparticles showed an initial burst release followed by a moderate and sustained release profile. Higher percentage of drugs from cumulative release can be achieved in the same prolonged time range. Therefore, PLGA nanoparticles modified by chitosan showed versatility of surface and a possible improvement in the efficacy of current PLGA-based drug delivery system.

摘要

PLGA(聚乳酸-羟基乙酸共聚物)载药系统表面的功能基团短缺一直阻碍其广泛应用,如被动靶向和与靶向分子偶联。在这项研究中,通过物理吸附和化学结合的方法将壳聚糖修饰到 PLGA 纳米颗粒上。通过改变壳聚糖溶液的 pH 值来调节表面电荷。壳聚糖引入后,PLGA 纳米颗粒表面的zeta 电位从负电荷变为正电荷,使药物载体对癌细胞更具亲和力。比较了 PLGA 纳米颗粒和壳聚糖修饰的 PLGA 纳米颗粒之间的功能基团。傅里叶变换红外光谱和 X 射线光电子能谱证实,壳聚糖修饰后 PLGA 纳米颗粒表面出现了胺基。修饰后的纳米颗粒表现出初始突释,随后是适度和持续的释放特征。在相同的延长时间范围内,可以实现更高比例的药物累积释放。因此,壳聚糖修饰的 PLGA 纳米颗粒显示出表面多功能性,并可能提高当前基于 PLGA 的药物输送系统的疗效。

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