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合成了一系列甲氧基聚乙二醇(MPEG)和聚(2-甲氧基乙基亚乙基磷酸酯)(PMOEEP)的两嵌段聚合物MPEG-b-PMOEEP,并研究了该嵌段聚合物对疏水性化疗药物紫杉醇(PTX)的增溶效果.以MPEG为引发剂、异辛酸亚锡为催化剂,对五元环状磷酸酯单体2-甲氧基乙氧基-1,3,2-二氧磷杂环戊烷(MOEEP)进行开环聚合获得了一系列两嵌段聚合物,用凝胶渗透色谱(GPC)和核磁共振波谱(NMR)对聚合物的结构进行了表征.两嵌段聚合物可在水中自组装形成以MPEG为壳PMOEEP为核的聚合物胶束状结构,并增强紫杉醇在水中的溶解度.研究结果表明紫杉醇的溶解度与聚合物的组成和浓度密切相关,随着PMOEEP链段长度的增加和MPEG链段长度的降低,紫杉醇在水中的溶解度增加;紫杉醇在水中的溶解度也随着聚合物浓度的增加而增加,且与聚合物的胶束化过程相关.该类嵌段聚合物能被磷酸二酯酶催化降解,且对乳腺癌细胞MCF-7没有显著细胞毒性,显示生物可降解性和良好的生物相容性.与此同时,经MPEG-b-PMOEEP增溶的紫杉醇显示良好的杀伤癌细胞的功能,证明这些两嵌段聚合物具有增溶紫杉醇并作为药物载体的良好潜力.
A series of MPEG-b-PMOEEP, a two-block polymer of methoxypolyethylene glycol (MPEG) and poly (2-methoxyethyl ethylene phosphite) The effect of segment polymer on the solubilization of hydrophobic chemotherapeutic agent paclitaxel (PTX) was studied.Methane as the initiator and stannous isooctanoate as catalyst were used to investigate the solubilization of 5-membered cyclic phosphate monomer, 2-methoxyethoxy-1, The ring-opening polymerization of 3,2-dioxaphospholane (MOEEP) gave a series of diblock polymers. The structure of the polymer was characterized by gel permeation chromatography (GPC) and nuclear magnetic resonance spectroscopy (NMR) The triblock copolymers can self-assemble in water to form micelles with MPEG as shell PMOEEP and enhance the solubility of paclitaxel in water.The results show that the solubility of paclitaxel is closely related to the composition and concentration of the polymer , The solubility of paclitaxel in water increased with the increase of length of PMOEEP segment and the decrease of MPEG segment length. The solubility of paclitaxel in water also increased with the increase of polymer concentration, Related such block polymers can be phosphodiesterase catalytic degradation, and breast cancer fine MCF-7 showed no significant cytotoxicity, showed biodegradability and good biocompatibility.At the same time, paclitaxel solubilized by MPEG-b-PMOEEP showed a good killing function of cancer cells, proving that these two block polymerization The substance has the potential to solubilize paclitaxel and act as a drug carrier.