首页|低临界胶束浓度PEGMA-b-PCL的制备及其药物缓释性能

低临界胶束浓度PEGMA-b-PCL的制备及其药物缓释性能

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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%.
Preparation and drug sustained-release properties of PEGMA-b-PCL with low critical micelle concentration
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.

RAFT polymerizationtwo-block polymerslow critical micelle concentrationdrug sustained-releasecurcumindrug materials

周国永、尹付琳、尹城武、王钰杰、陈雨鑫、刘超、成琳、杜海军

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贵州民族大学 化学工程学院,贵州 贵阳 550025

贵州民族大学 民族医药学院,贵州 贵阳 550025

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

国家自然科学基金贵州省省级科技计划贵州省高等学校绿色化学与资源环境创新团队项目贵州民族大学科研项目

82060714黔科合基础-ZK[2022]一般216黔科技[2022]13号GZMUZK[2021]YB09

2024

10.13550/j.jxhg.20230406

精细化工
大连化工研究院设计院 中国化工学会精细化工专业委员会 辽宁省化工研究院

精细化工

CSTPCD北大核心
影响因子：0.557
ISSN：1003-5214
年,卷(期)：2024.41(6)
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