School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
Int J Pharm. 2012 Feb 28;423(2):195-201. doi: 10.1016/j.ijpharm.2011.12.017. Epub 2011 Dec 17.
Amino poly(glycerol methacrylate)s (PGOHMAs) were synthesized from linear or star-shaped poly(glycidyl methacrylate)s (PGMA)s via ring opening reactions with 1,2-ethanediamine, 1,4-butanediamine and diethylenetriamine, respectively. The resulting cationic polymers were employed to form polyelectrolyte complexes (PECs) with insulin. Parameters influencing complex formation were investigated by dynamic light scattering (DLS). PECs in the size range of 100-200 nm were obtained under optimal conditions, i.e., the pH value of PECs was 5.58-6.27, the concentration of NaCl was 0.02 mol/L, and insulin-polymer weight ratio was 0.8. The insulin association efficiency (AE) of current system increased with zeta potentials of PECs. Circular dichroism (CD) analysis corroborated that the structure of insulin in the PEC nanoparticles was preserved after lyophilization. Fourier transform infrared (FT-IR) and X-ray diffraction (XRD) experiments demonstrated that weak physical interactions between insulin and amino PGOHMAs play an important role in the formation of PECs. The release of insulin depends on both structure and architecture of amino PGOHMAs. These PECs would be potentially useful for mucosal administration.
氨基酸聚（甘油甲基丙烯酸酯）（PGOHMAs）是通过线性或星形聚（甲基丙烯酸缩水甘油酯）（PGMA）与 1,2-乙二胺、1,4-丁二胺和二乙烯三胺分别开环反应合成的。所得阳离子聚合物与胰岛素形成聚电解质复合物（PECs）。通过动态光散射（DLS）研究了影响复合物形成的参数。在最佳条件下获得了粒径为 100-200nm 的 PECs，即 PECs 的 pH 值为 5.58-6.27，NaCl 的浓度为 0.02mol/L，胰岛素-聚合物的重量比为 0.8。该体系中胰岛素的结合效率（AE）随 PEC 的zeta 电位的增加而增加。圆二色性（CD）分析证实，胰岛素在冻干后的 PEC 纳米粒中的结构得以保留。傅立叶变换红外（FT-IR）和 X 射线衍射（XRD）实验表明，胰岛素与氨基酸 PGOHMAs 之间的弱物理相互作用对 PECs 的形成起着重要作用。胰岛素的释放取决于氨基酸 PGOHMAs 的结构和架构。这些 PECs可能对粘膜给药有用。
