壳聚糖季铵盐纳米粒子的制备、表征及其缓释蛋白质药物性能

Preparation and Controlled Release of Quaternized Chitosan Nanoparticles as a Protein Carrier

用N (2 羟基)丙基 3 甲基氯化铵壳聚糖(QC)与三聚磷酸钠(TPP)离子交联制备了一种新型的纳米粒子,粒径约为110～180nm.经傅立叶红外光谱表征,发现该纳米粒子与QC的结构比较发生了较大改变,形成了较强的分子间氢键,且TPP连接到了纳米粒子QC上的铵基位点.以牛血清白蛋白(BSA)为模型药物,增加BSA的初始浓度可提高纳米粒子对BSA的包封率.交联剂的浓度从0.5g·L-1增加到0.7g·L-1时,纳米粒子对BSA的包封率可从46.7%提高到90%,且载药QC纳米粒子体外释放实验在初期的突释量明显减小(从43%减至28%),载药纳米粒子突释之后均呈现缓慢而持续的释放.

N-(2-hydroxyl) propyl-3-trimethyl ammonium chitosan chloride (QC) was water-soluble derivative of chitosan, synthesized by the reaction between glycidyl-trimethyl-ammonium chloride and chitosan. QC nanoparticles with 110-180 nm in size have been formed based on ionic gelation process of QC and sodium tripolyphosphate (TPP). FTIR confirmed tripolyphosphoric groups of TPP linked with ammonium groups of QC in the nanoparticles. Bovine serum albumin (BSA), as a model protein drug, was incorporated into the QC nanoparticles, its encapsulation efficiency was obviously increased with increase of initial BSA concentration. In vitro release studies showed a burst effect and a slow and continuous release followed. Increasing TPP concentration from 0.5 g·L^(-1) to 0.7 g·L^(-1) promoted encapsulation efficiency from 46.7% to 90%, and decreased burst release.