低临界胶束浓度PEGMA-b-PCL的制备及其药物缓释性能
Preparation and drug sustained-release properties of PEGMA-b-PCL with low critical micelle concentration
周国永 1尹付琳 1尹城武 1王钰杰 1陈雨鑫 1刘超 1成琳 2杜海军1
作者信息
- 1. 贵州民族大学 化学工程学院,贵州 贵阳 550025
- 2. 贵州民族大学 民族医药学院,贵州 贵阳 550025
- 折叠
摘要
以ε-己内酯(ε-CL)为疏水链段、聚乙二醇甲醚甲基丙烯酸酯(PEGMA)为亲水链段、4-氰基-4-[(十二烷基硫烷基硫代羰基)硫烷基]戊醇(CDPA)为可逆加成-断裂链转移(RAFT)试剂、甲苯为溶剂,在N2氛围、80℃、反应 24 h的条件下,通过RAFT聚合法制备了两嵌段共聚物(PEGMA-b-PCL).将其自组装为胶束,作为纳米药物载体用于负载姜黄素(Cur).采用FTIR、1HNMR、GPC、SEM、DLS对PEGMA-b-PCL进行了表征,测试了胶束载体的载药和释药性能.结果表明,两嵌段共聚物数均相对分子质量范围为 1478～7318,其具有较低的临界胶束浓度(在pH=5.0～7.4,范围为0.920～1.600 mg/L).胶束载体粒径范围为68.34～186.93 nm.当n(CDPA)∶n(ε-CL)=1∶200时,胶束载药率和包封率最高,可达12.05%±0.29%和75.26%±2.41%.在不同pH环境下,药物缓释性能可达15 d,其中pH=5.0时的累积释药率最高,可达38.20%.
Abstract
Two-block copolymers(PEGMA-b-PCL)were prepared by reversible addition and break chain transfer(RAFT)polymerization of hydrophobic ε-caprolactone(ε-CL)and hydrophilic polyethylene glycol methyl ether methacrylate(PEGMA),with 4-cyano-4-[(dodecylsulfanylthiocarbonyl)sulfanyl]pentanol(CDPA)as RAFT reagent and toluene as solvent under N2 atmosphere at 80℃for 24 h.The PEGMA-b-PCL micelles were then formed via self-assembly and used as nanomedical carriers for curcumin(Cur).The PEGMA-b-PCL were characterized by FTIR,1HNMR,GPC,SEM and DLS,and the drug loading and release properties of micelle carriers were analyzed.The results showed that the PEGMA-b-PCL exhibited a number-average relative molecular mass ranging from 1478～7318,and a low critical micelle concentration of 0.920 to 1.600 mg/L at pH=5.0～7.4.The micelle carriers,with a particle size of 68.34～186.93 nm,displayed the highest drug loading and encapsulation rate of 12.05%±0.29%and 75.26%±2.41%,respectively at n(CDPA)∶n(ε-CL)=1∶200.Under different pH conditions,the drug slow-release performance of the micellar carrier could reach 15 d,while the cumulative release rate could reach 38.20%at pH=5.0.
关键词
RAFT聚合/两嵌段共聚物/低临界胶束浓度/药物缓释/姜黄素/医药原料Key words
RAFT polymerization/two-block polymers/low critical micelle concentration/drug sustained-release/curcumin/drug materials引用本文复制引用
基金项目
国家自然科学基金(82060714)
贵州省省级科技计划(黔科合基础-ZK[2022]一般216)
贵州省高等学校绿色化学与资源环境创新团队项目(黔科技[2022]13号)
贵州民族大学科研项目(GZMUZK[2021]YB09)
出版年
2024
NETL
NSTL
万方数据