Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
J Biomater Sci Polym Ed. 2010;21(6-7):759-70. doi: 10.1163/156856209X441991.
Poly(alpha,beta-[N-(2-hydroxyethyl)-L-aspartamide])-folate (PHEA-FA) was synthesized by linking FA to a poly(alpha,beta-[N-(2-hydroxyethyl)-L-aspartamide]) (PHEA) backbone. The chemical structure of PHEA-FA was characterized by (1)H-NMR and FT-IR. The molecular weights of the polymers were determined by combined size-exclusion chromatography and multiangle laser light scattering (SEC-MALLS) analysis. Due to the incorporation of FA, PHEA-FA exhibited pH-sensitive aggregation behavior in aqueous media. As characterized by UV-Vis spectroscopy and fluorescence spectroscopy, PHEA-FA could self-assemble to form aggregates in acidic and neutral aqueous solutions, and became soluble in a basic solution. The potential application of PHEA-FA in drug delivery was explored. Drug-loaded PHEA-FA nanoparticles were fabricated and the in vitro drug release of the drug-loaded nanoparticles was investigated. Transmission electron microscopy (TEM) showed that the nanoparticles exhibited a spherical morphology with particle sizes <100 nm. The in vitro study showed PHEA-FA exhibited enhanced cell uptake on the folate-receptor-positive cells because of the folate-mediated targeting.
聚（α，β-[N-（2-羟乙基）-L-天冬酰胺]）-叶酸（PHEA-FA）通过将 FA 连接到聚（α，β-[N-（2-羟乙基）-L-天冬酰胺]）（PHEA）主链上合成。通过（1）H-NMR 和 FT-IR 对 PHEA-FA 的化学结构进行了表征。通过组合的尺寸排阻色谱和多角度激光光散射（SEC-MALLS）分析确定了聚合物的分子量。由于 FA 的掺入，PHEA-FA 在水介质中表现出 pH 敏感的聚集行为。通过紫外可见光谱和荧光光谱表征，PHEA-FA 可以在酸性和中性水溶液中自组装形成聚集体，并在碱性溶液中溶解。探讨了 PHEA-FA 在药物传递中的潜在应用。制备了载药 PHEA-FA 纳米粒，并研究了载药纳米粒的体外药物释放。透射电子显微镜（TEM）显示，纳米粒呈现出小于 100nm 的球形形态。体外研究表明，由于叶酸介导的靶向作用，PHEA-FA 在叶酸受体阳性细胞中表现出增强的细胞摄取。
