School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
Eur J Pharm Sci. 2012 Jan 23;45(1-2):65-72. doi: 10.1016/j.ejps.2011.10.025. Epub 2011 Nov 9.
Poly(glycerol methacrylate)s (PGOHMAs) were successfully synthesized via the hydrolysis of the epoxy groups on linear and/or star-shaped poly(glycidyl methacrylate)s (PGMAs). Further modification of the hydroxyl groups on PGOHMAs with succinic anhydride (SA) or 1,2-cyclohexanedicarboxylic anhydride (CDA) resulted in a new type of polyacid polymer, namely, PGOHMACOOH for short, which was then employed to prepare pH-sensitive assemblies using dialysis method. The carboxylated polymers were quite effective in the encapsulation of doxorubicin hydrochloride (DOX) by electrostatic interaction. Compared with poly(acrylic acid) (PAA), the star-shaped PGOHMA modified with CDA exhibited higher encapsulation efficiency and loading capacity, as well as better pH-responsive release profile. Scanning electron microscope images showed that the polymeric nanoparticles before and after encapsulation of DOX were spherical in shape. The encapsulation efficiency, loading capacity and release properties of these polymers were found to rely on their backbone architectures and the type of carboxylated functionalities. By fine-tuning these factors to achieve optimal properties, such type of polymeric materials holds promise as an attractive and effective drug delivery vehicle.
聚（甘油甲基丙烯酸酯）（PGOHMAs）是通过线性和/或星形聚（甲基丙烯酸缩水甘油酯）（PGMAs）上的环氧基团的水解成功合成的。PGOHMAs 上的羟基与琥珀酸酐（SA）或 1,2-环己烷二甲酸酐（CDA）进一步修饰得到了一种新型聚酸聚合物，简称 PGOHMACOOH，然后采用透析法制备 pH 敏感组装体。该羧化聚合物通过静电相互作用非常有效地包封盐酸阿霉素（DOX）。与聚丙烯酸（PAA）相比，用 CDA 修饰的星形 PGOHMA 表现出更高的包封效率和载药量，以及更好的 pH 响应释放特性。扫描电子显微镜图像显示，DOX 包封前后的聚合物纳米粒子呈球形。这些聚合物的包封效率、载药量和释放性能取决于其主链结构和羧基化功能团的类型。通过精细调整这些因素以达到最佳性能，这种类型的聚合物材料有望成为一种有吸引力且有效的药物输送载体。
