文章摘要
聚乙二醇-b-聚乳酸末端官能团的合成及在卡巴他赛载药体系中的应用
Poly(ethylene glycol)-b-Poly(lactic acid) Terminal Modification and Application in Cabazitaxel Take Medicine System
  
DOI:10.16865/j.cnki.1000-7555.2018.06.007
中文关键词: 聚乙二醇-b-聚乳酸  末端改性  化学键合  π-π堆叠效应  相似相容
英文关键词: poly(ethylene glycol)-b-poly(lactic acid)  terminal modification  chemical bonding  π-π stacking  similar dissolve mutually theory
基金项目:北京建筑大学科研基金项目KYJJ2017020
作者单位
于小杰1,2, 伍一波1, 毛 静3, 金玉顺1, 李树新1, 杨 丹1, 王 浩1 1. 北京石油化工学院材料科学与工程学院 北京市特种弹性体重点实验室北京 1026172. 北京化工大学 材料科学与工程学院, 北京 100029 3. 北京建筑大学 北京建筑结构与环境修复功能材料重点实验室北京 102612 
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中文摘要:
      为了提高聚乙二醇-b-聚乳酸(PEG-PLA)与药物卡巴他赛(Cabazitaxel)的相容性以及载药能力,对PEG-PLA进行末端官能团改性,一方面通过化学键合的方法,在PEG-PLA末端接枝药物卡巴他赛;另一方面在PEG-PLA的末端实现官能团的修饰,引入苯环(PEG-PLA-Bz)、乙酰基(PEG-PLA-Ac),通过π-π堆叠效应和相似相溶原理来提高PEG-PLA的载药能力。采用核磁共振谱图(1H-NMR)对末端官能化的目标产物进行分析表征,利用高效液相色谱法(HPLC)和药物血浆释放实验测定胶束的包封率、载药量以及在血浆中的药物浓度。结果表明,通过π-π堆叠形成的胶束的包封率最高,可以达到71.5%,相对分子质量分布较均匀,而且药物缓释作用最好,在360 min后血浆中药物的浓度为2.2 μg/mL。
英文摘要:
      To increase the drug-loading capacity and stability of poly(ethylene glycol)-b-poly(lactic acid) (PEG-b-PLA),a terminal modification method was utilized to load cabazitaxel (CBT). Effective ways to control drugs release from micelles was conjugating drugs to polymeric materials or cross-linking polymers by chemical reaction or through similar dissolve mutually theory for combination of polymers and drugs. The target product of terminal functionalization was characterized by 1H-NMR. The micelles encapsulation efficiency, drug loading, and drug concentration in plasma were determined by HPLC and drug plasma release assay. In conclusion, the π-π stacking effect introduced by aromatic groups increases the stability and loading capacity of polymeric micelles. The micelles have a drug loading capacity up to 71.5% for CBT. Test the plasma drug concentration, the plasma drug concentration of PEG-PLA-Bz is the best, and the drug concentration in the plasma is 2.2 μg/mL after 360 min. These results suggest that the micelles based on π-π stacking hold great potential as sustained delivery system.
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