Hu Xiuli, Liu Shi, Chen Xuesi, Mo Guojun, Xie Zhigang, Jing Xiabin
State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, PR China.
Biomacromolecules. 2008 Feb;9(2):553-60. doi: 10.1021/bm701092j. Epub 2008 Jan 22.
A new biodegradable amphiphilic block copolymer, poly(ethylene glycol)-b-poly(L-lactide-co-9-phenyl-2,4,8,10-tetraoxaspiro[5,5]undecan-3-one) [PEG-b-P(LA-co-PTO)], was successfully prepared by ring-opening polymerization (ROP) of L-lactide (LA) and functionalized carbonate monomer 9-phenyl-2,4,8,10-tetraozaspiro[5,5]undecan-3-one (PTO) in the presence of monohydroxyl poly(ethylene glycol) as macroinitiator using Sn(Oct)2 as catalyst. NMR, FT-IR, and GPC studies confirmed the copolymer structure. It could self-assemble into micelles in aqueous solution with critical micelle concentration (CMC) in the magnitude of mg/L, which changed with the composition of the copolymer. After catalytic hydrogenation, copolymers with active hydroxyl groups were obtained. Adhesion and proliferation of Vero cells on the copolymer films showed that the synthesized copolymers were good biocompatible materials. In vitro degradation of the copolymer before and after deprotection was investigated in the presence of proteinase K. The free hydroxyl groups on the copolymers were capable of further modification with biotin. This new amphiphilic block copolymer has great potential for both drug encapsulation and conjugate because of its low CMC and the presence of active hydroxyl groups.
一种新型可生物降解的两亲性嵌段共聚物，聚（乙二醇）-b-聚（L-丙交酯-co-9-苯基-2,4,8,10-四氧杂螺[5,5]十一烷-3-酮）[PEG-b-P(LA-co-PTO)]，通过以单羟基聚（乙二醇）为大分子引发剂，在Sn(Oct)2作为催化剂的存在下，对L-丙交酯（LA）和官能化碳酸酯单体9-苯基-2,4,8,10-四氧杂螺[5,5]十一烷-3-酮（PTO）进行开环聚合（ROP）成功制备。核磁共振（NMR）、傅里叶变换红外光谱（FT-IR）和凝胶渗透色谱（GPC）研究证实了共聚物结构。它能在水溶液中自组装成胶束，临界胶束浓度（CMC）在mg/L量级，且随共聚物组成而变化。催化氢化后，得到了带有活性羟基的共聚物。Vero细胞在共聚物薄膜上的黏附和增殖表明合成的共聚物是良好的生物相容性材料。在蛋白酶K存在的情况下，研究了脱保护前后共聚物的体外降解。共聚物上的游离羟基能够用生物素进一步修饰。这种新型两亲性嵌段共聚物因其低CMC和活性羟基的存在，在药物包封和偶联方面都具有巨大潜力。
