Department of Polymer.Nano Science and Technology, Polymer Fusion Research Center, Chonbuk National University, Dukjin, Jeonju, Korea.
Biomacromolecules. 2010 Mar 8;11(3):555-60. doi: 10.1021/bm901409k.
One of major challenges in the drug delivery lies in the development of nanoparticles that are effectively delivered to targeted cells and release their payload over an extended period to achieve a clinical response. In this paper, we report a new family of biocompatible and biodegradable polymer, termed polyoxalate that degrades hydrolytically into nontoxic byproducts. Polyoxalate was synthesized from a simple one-step polymerization reaction of 1,4-cyclohexanedimethanol and oxalyl chloride and had a MW of approximately 11000 Da. This polymer was designed to degrade by water hydrolysis into 1,4-cyclohexanedimethanol and oxalic acid, which can be easily removed from a body. Polyoxalate had a hydrophobic backbone and was formulated into nanoparticles with a mean diameter of 600 nm, which is suitable for drug delivery involving phagocytosis by macrophages. Polyoxalate nanoparticles were readily taken up by RAW 264.7 macrophage cells and HEK (human embryonic kidney) 293 cells and exhibited a minimal cytotoxicity in a time- and dose-dependent manner. In comparison with PLGA nanoparticles, polyoxalate nanoparticles had a significantly higher cell viability. We anticipated that the ease of synthesis and excellent biocompatibility make polyoxalate highly potent for numerous applications in drug delivery.
在药物输送中,一个主要的挑战在于开发能够有效地递送到靶细胞并在延长的时间内释放其有效载荷以实现临床反应的纳米颗粒。在本文中,我们报告了一类新型的生物相容性和可生物降解聚合物,称为聚草酸酯,它可通过水解逐渐降解为无毒的副产物。聚草酸酯是通过 1,4-环己烷二甲醇和草酰氯的简单一步聚合反应合成的,分子量约为 11000 Da。该聚合物的设计目的是通过水解水化为 1,4-环己烷二甲醇和草酸,这可以很容易地从体内清除。聚草酸酯具有疏水主链,并被配制成平均直径为 600nm 的纳米颗粒,适用于涉及巨噬细胞吞噬作用的药物输送。聚草酸酯纳米颗粒很容易被 RAW 264.7 巨噬细胞和 HEK(人胚肾)293 细胞摄取,并表现出时间和剂量依赖性的最小细胞毒性。与 PLGA 纳米颗粒相比,聚草酸酯纳米颗粒具有更高的细胞活力。我们预计,其易于合成和出色的生物相容性使其在药物输送的众多应用中具有很高的潜力。