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用于药物递送的两亲性超支化核/壳型聚合物纳米载体平台的设计

Design of an amphiphilic hyperbranched core/shell-type polymeric nanocarrier platform for drug delivery.

作者信息

Bal ÖztÜrk Ayça, OĞuz Nesrin, Tekarslan Şahİn Hande, Emİk Serkan, AlarÇİn Emine

机构信息

Department of Analytical Chemistry, Faculty of Pharmacy, İstinye University, İstanbul Turkey.

Department of Stem Cell and Tissue Engineering, Institute of Health Sciences, İstinye University, İstanbul Turkey.

出版信息

Turk J Chem. 2020 Apr 1;44(2):518-534. doi: 10.3906/kim-1910-35. eCollection 2020.

Abstract

An amphiphilic core/shell-type polymer-based drug carrier system (HPAE- PCL-b -MPEG), composed of hyperbranched poly(aminoester)-based polymer (HPAE) as the core building block and poly(ethylene glycol)-b - poly(ε-caprolactone) diblock polymers (MPEG-b -PCL) as the shell building block, was designed. The synthesized polymers were characterized with FTIR, 1 H NMR, 13 C NMR, and GPC analysis. Monodisperse HPAE-PCL-b - MPEG nanoparticles with dimensions of < 200 nm and polydispersity index of < 0.5 were prepared by nanoprecipitation method and characterized with SEM, particle size, and zeta potential analysis. 5-Fluorouracil was encapsulated within HPAE-PCL-b -MPEG nanoparticles. In vitro drug release profiles and cytotoxicity of blank and 5-fluorouracil-loaded nanoparticles were examined against the human colon cancer HCT116 cell line. All results suggest that HPAE-PCL-b - MPEG nanoparticles offer an alternative and effective drug nanocarrier system for drug delivery applications.

摘要

设计了一种两亲性核/壳型聚合物基药物载体系统(HPAE-PCL-b-MPEG),其由作为核心构建单元的超支化聚(氨基酯)基聚合物(HPAE)和作为壳层构建单元的聚(乙二醇)-b-聚(ε-己内酯)二嵌段聚合物(MPEG-b-PCL)组成。通过傅里叶变换红外光谱(FTIR)、氢核磁共振(1H NMR)、碳核磁共振(13C NMR)和凝胶渗透色谱(GPC)分析对合成的聚合物进行了表征。采用纳米沉淀法制备了尺寸小于200 nm且多分散指数小于0.5的单分散HPAE-PCL-b-MPEG纳米颗粒,并通过扫描电子显微镜(SEM)、粒度分析和zeta电位分析对其进行了表征。将5-氟尿嘧啶包封在HPAE-PCL-b-MPEG纳米颗粒中。考察了空白纳米颗粒和负载5-氟尿嘧啶的纳米颗粒对人结肠癌HCT116细胞系的体外药物释放曲线和细胞毒性。所有结果表明,HPAE-PCL-b-MPEG纳米颗粒为药物递送应用提供了一种替代的有效药物纳米载体系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cef/7671224/ca2f25a383df/turkjchem-44-518-fig001.jpg

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