PCFM Lab, GD HPPC Lab, School of Chemistry, Sun Yat-sen University, Guangzhou, Guangdong 510275, China.
PCFM Lab, GD HPPC Lab, School of Chemistry, Sun Yat-sen University, Guangzhou, Guangdong 510275, China.
Mater Sci Eng C Mater Biol Appl. 2020 Aug;113:110979. doi: 10.1016/j.msec.2020.110979. Epub 2020 Apr 19.
In this article, a simvastatin loaded pentaerythritol tetra(3-mercaptopropionate)-allylurea-poly(ethylene glycol) (SIM-loaded PETMP-AU-PEG) polymer with excellent biocompatibility by means of in-situ loading method was synthesized. The presence of the imine bonds has given the polymer system an excellent response performance to weak acidic environment. Specifically, for the SIM-loaded polymer, the simvastatin cumulative release dose is only 2.2% in the first 2 h, and the first 32 h of the cumulative release dose is less than 10% in pH 7.4; However, in pH 6.0, the first 2 h of the cumulative release dose is 65.2%, and the first 32 h of the cumulative release dose is almost 100%. MC3T3-E1 osteoblast cell culture experiments show that the SIM-loaded polymer at pH 6.0 can accelerate the proliferation of osteoblasts significantly, which is expected to promote the rapid proliferation of bone cells in clinical applications and accelerate the healing of the lesion region.
本文通过原位负载法合成了一种具有良好生物相容性的载辛伐他汀的季戊四醇四（3-巯基丙酸酯）-烯丙基脲-聚乙二醇（SIM-负载的 PETMP-AU-PEG）聚合物。亚胺键的存在赋予了聚合物体系对弱酸性环境的优异响应性能。具体来说，对于载辛伐他汀的聚合物，在 pH 7.4 条件下，前 2 h 的辛伐他汀累积释放剂量仅为 2.2%，前 32 h 的累积释放剂量小于 10%；然而，在 pH 6.0 条件下，前 2 h 的累积释放剂量为 65.2%，前 32 h 的累积释放剂量几乎为 100%。MC3T3-E1 成骨细胞培养实验表明，pH 6.0 下的载 SIM 聚合物能够显著促进成骨细胞的增殖，有望在临床应用中促进骨细胞的快速增殖，加速病变区域的愈合。
