不同结构PEG-PCL共聚物纳米粒的制备及质量评价

Preparation of PEG-PCL copolymer nanoparticles with different structures and their quality evaluation

为了比较聚乙二醇-聚己内酯(PEG-PCL)不同结构共聚物纳米粒的性质,采用开环聚合反应制备PCL-PEG-PCL和mPEG-b-PCL共聚物,通过FT-IR,1H-NMR和GPC进行结构确证,利用分子自组装技术分别形成了“蘑菇”结构和“刷”结构载姜黄素(CUR)纳米粒共聚物,对其性质进行了研究。结果表明:CUR以无定型态存在于纳米粒中,纳米粒形貌为球形核壳结构且分布均匀;受共聚物结构的影响,“蘑菇”结构纳米粒具有较小的平均粒径(105.71±3.20)nm、较高的载药量和包封率;PCL-PEG-PCL纳米粒表面形成了致密的PEG层,能有效防止蛋白质吸附,在体内具有良好的稳定性;“刷”结构纳米粒具有较低的临界胶束浓度(CMC)和良好的缓释性能,对HepG-2细胞增殖有较高的抑制作用。因此,研究载药纳米粒可为药物递送系统的选择以及不同结构纳米粒的临床应用提供参考。

In order to compare the properties of polyethylene glycol-polycaprolactone(PEG-PCL)with different structures,the PCL-PEG-PCL and mPEG-b-PCL copolymers are obtained by ring-opening polymerization method and characterized by FT-IR,1H-NMR and GPC.The curcumin-loaded nanoparticles of"mushroom"and"brush"are prepared via self-assembly method,and the properties of the two structural nanoparticles are studied.The results show that CUR is encapsulated into the nanoparticles with an amorphous state;the nanoparticles show a smooth surface with core-shell structures and good dispersibility.Influenced by the structure of the copolymer,the"mushroom"nanoparticles have a smaller average particle size of(105.71±3.20)nm,a higher drug loading and encapsulation efficiency.Since the surface of the PCL-PEG-PCL nanoparticles forms a dense PEG-layer,protein resistance studies show that the"mushroom"nanoparticles are good in vivo stability."Brush"nanoparticles have a lower CMC date and better sustained release properties,and have a higher inhibitory effect on HepG-2 cancer cell proliferation.The study of drug-loaded nanoparticles can provide reference for drug delivery system selection and clinical application of nanoparticles with different structures.