Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, ON, Canada.
Colloids Surf B Biointerfaces. 2013 Jan 1;101:405-13. doi: 10.1016/j.colsurfb.2012.07.015. Epub 2012 Jul 20.
This work focused on the design of new pH-responsive nanoparticles for controlled delivery of anticancer drug doxorubicin (Dox). Nanoparticles of poly(methacrylic acid)-polysorbate 80-grafted starch (PMAA-PS 80-g-St) were synthesized by using a one-pot method that enabled simultaneous grafting of PMAA and PS 80 onto starch and nanoparticle formation in an aqueous medium. The particles were characterized by FTIR, (1)H NMR, TEM, DLS, and potentiometric titration. Dox loading and in vitro release from the nanoparticles were investigated. The FTIR and (1)H NMR confirmed the chemical composition of the graft terpolymer. The nanoparticles were relatively spherical with narrow size distribution and porous morphology. They exhibited pH-dependent swelling in a physiological pH range. The particle size and magnitude of phase transition were dependent on polymer composition and formulation parameters such as concentrations of surfactant and cross-linking agent and total monomer concentration. The nanoparticles with optimized compositions showed high loading capacity for Dox and sustained Dox release. The results suggest that the new pH-responsive terpolymer nanoparticles are useful in controlled drug delivery.
这项工作专注于设计新的 pH 响应性纳米粒子，用于控制抗癌药物阿霉素（Dox）的递送。通过一锅法合成了聚（甲基丙烯酸）-聚山梨酯 80-接枝淀粉（PMAA-PS 80-g-St）纳米粒子，该方法能够在水介质中同时将 PMAA 和 PS 80 接枝到淀粉上并形成纳米粒子。通过傅里叶变换红外光谱（FTIR）、（1）H 核磁共振（NMR）、透射电子显微镜（TEM）、动态光散射（DLS）和电位滴定对颗粒进行了表征。研究了纳米粒子对 Dox 的负载和体外释放。FTIR 和（1）H NMR 证实了接枝共聚物的化学组成。纳米粒子具有相对球形的形状、较窄的粒径分布和多孔的形态。它们在生理 pH 范围内表现出 pH 依赖性溶胀。粒径和相变幅度取决于聚合物组成和制剂参数，如表面活性剂和交联剂的浓度以及总单体浓度。具有优化组成的纳米粒子对 Dox 具有高负载能力和持续的 Dox 释放。结果表明，新型 pH 响应性三嵌段共聚物纳米粒子在控制药物递送方面具有应用价值。
