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基于水溶性壳聚糖-聚(L-天冬氨酸)-聚乙二醇的聚电解质纳米颗粒用于蛋白质的可控释放。

Polyelectrolyte nanoparticles based on water-soluble chitosan-poly(L-aspartic acid)-polyethylene glycol for controlled protein release.

作者信息

Shu Shujun, Zhang Xinge, Teng Dayong, Wang Zhen, Li Chaoxing

机构信息

The Key laboratory of Functional Polymer Material of Ministry of Education, Institute of Polymer Chemistry, Nankai University, 94# Weijin Road, Tianjin 300071, PR China.

出版信息

Carbohydr Res. 2009 Jul 6;344(10):1197-204. doi: 10.1016/j.carres.2009.04.018. Epub 2009 Apr 20.

DOI:10.1016/j.carres.2009.04.018
PMID:19508912
Abstract

Water-soluble chitosan (WSC)-poly(L-aspartic acid) (PASP)-polyethylene glycol (PEG) nanoparticles (CPP nanoparticles) were prepared spontaneously under quite mild conditions by polyelectrolyte complexation. These nanoparticles were well dispersed and stable in aqueous solution, and their physicochemical properties were characterized by turbidity, FTIR spectroscopy, dynamic light scattering (DLS), transmission electron microscope (TEM), and zeta potential. PEG was chosen to modify WSC-PASP nanoparticles to make a protein-protective agent. Investigation on the encapsulation efficiency and loading capacity of the bovine serum albumin (BSA)-loaded CPP nanoparticles was also conducted. Encapsulation efficiency was obviously decreased with the increase of initial BSA concentration. Furthermore, its in vitro release characteristics were evaluated at pH 1.2, 2.5, and 7.4. In vitro release showed that these nanoparticles provided an initial burst release, followed by a slowly sustained release for more than 24 h. The BSA released from CPP nanoparticles showed no significant conformational change compared with native BSA, which is superior to the BSA released from nanoparticles without PEG. A cell viability study suggested that the nanoparticles had good biocompatibility. This nanoparticle system was considered promising as an advanced drug delivery system for the peptide and protein drug delivery.

摘要

通过聚电解质络合在相当温和的条件下自发制备了水溶性壳聚糖(WSC)-聚(L-天冬氨酸)(PASP)-聚乙二醇(PEG)纳米颗粒(CPP纳米颗粒)。这些纳米颗粒在水溶液中分散良好且稳定,通过浊度、傅里叶变换红外光谱(FTIR)、动态光散射(DLS)、透射电子显微镜(TEM)和zeta电位对其理化性质进行了表征。选择PEG修饰WSC-PASP纳米颗粒以制备蛋白质保护剂。还对负载牛血清白蛋白(BSA)的CPP纳米颗粒的包封率和载药量进行了研究。随着初始BSA浓度的增加,包封率明显降低。此外,在pH 1.2、2.5和7.4条件下评估了其体外释放特性。体外释放表明,这些纳米颗粒呈现初始突释,随后缓慢持续释放超过24小时。与天然BSA相比,从CPP纳米颗粒释放的BSA没有明显的构象变化,这优于从不含PEG的纳米颗粒释放的BSA。细胞活力研究表明,这些纳米颗粒具有良好的生物相容性。该纳米颗粒系统被认为有望成为用于肽和蛋白质药物递送的先进药物递送系统。

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