基于聚半乳糖醛酸的聚合物胶束制备及性能  

Preparation and Properties of Polymer Micelles Based on Polygalacturonic Acid

作　　者：刘银春 张永勤[1] 董静文 刘芳[1] 刘建瑞 LIU Yinchun;ZHANG Yongqin;DONG Jingwen;LIU Fang;LIU Jianrui(College of Chemical Engineering,Qingdao University of Science and Technology,Qingdao 266042,Shandong,China)

机构地区：[1]青岛科技大学化工学院,山东青岛266042

出　　处：《功能高分子学报》2024年第4期347-355,共9页Journal of Functional Polymers

基　　金：山东省重点研发计划项目(2019GSF107081)。

摘　　要：以胱胺(CYS)和脱氧胆酸(DOCA)为原料合成了胱胺修饰的脱氧胆酸(CD),再将CD的氨基(―NH_(2))与聚半乳糖醛酸(PGA)的羧基(―COOH)通过酰胺化反应制得PGA-g-CD聚合物,并自组装为胶束。通过调节n(―NH_(2))∶n(―COOH)对胶束载药性能进行调控。测试了聚合物的结构及聚合物胶束的载药和释药性能。结果表明,最佳投料比为n(―NH_(2))∶n(―COOH)=1.3∶1,在该条件下,CD在聚合物中取代度为31%,临界胶束浓度为0.025 mg/mL,胶束载药量达11.53%,载药胶束粒径和粒径多分散系数分别为(296.1±0.3)nm和0.101±0.053,在还原性环境中36 h的释药量可达78.8%,体现良好的还原响应性。Cystamine(CYS)and deoxycholic acid(DOCA)were used as raw materials to synthesize cystamine modified deoxycholic acid(CD),and then the amino group(―NH_(2))of CD and the carboxyl group(―COOH)of polygalacturonic acid(PGA)were synthesized into PGA-g-CD polymer through amidation reaction.The polymer was self-assembled into micelles in the aqueous solution through dialysis.Doxorubicin(DOX)was used as a model drug,it was encapsulated in the hydrophobic core of the micelles.By regulating the feed ratio of n(―NH_(2))∶n(―COOH),the drug-loading performance of the micelles was controlled.The polymers were characterized by 1H-nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy,and the substitution degree(DS)of CD in the polymer was measured in sequence.The structure,drug loading and drug release properties of the polymer micelles were tested using transmission electron microscope,dynamic light scattering and Zeta potential analyzer,etc.The optimal feed ratio is n(―NH_(2))∶n(―COOH)=1.3∶1.Under this condition,the DS in the polymer is 31%,and the critical micelle concentration is 0.025 mg/mL.The drug loading capacity and encapsulation efficiency of the micelles reach 11.53%and 60.68%,respectively.The particle sizes of the polymer micelles and the drug-loaded micelles are(208.5±4.1)nm and(296.1±0.3)nm,respectively.And the polydispersity index values are 0.215±0.008 and 0.101±0.053,respectively.Under the reductive condition,the cumulative drug release amount within 36 h reach 78.8%,compared to 22.9%in the non-reductive environment,showing good reductive responsiveness.

关 键 词：聚半乳糖醛酸 聚合物 胶束 还原敏感 释药 

分 类 号：O63[理学—高分子化学]