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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1.贵州民族大学化学工程学院;2.贵州民族大学 化学工程学院;3.贵州民族大学 民族医药学院

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国家自然科学(82060714);贵州省省级科技计划项目(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(黔科技[2022]13号);贵州民族大学科研项目(GZMUZK[2021]YB09)资助。


Preparation of the lower CMC nanocarrier PEGMA-b-PCL and its drug sustained-release properties
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1.College of Chemical Engineering,Guizhou Minzu University;2.School ofSEthnic-Minority Medicine,Guizhou Minzu University

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    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-[(十二烷基硫基硫羰基)硫基]戊酸(CDPA)为可逆加成-断裂链转移(RAFT)试剂,在以甲苯为溶剂、N2氛围、80 ℃、反应24 h的条件下,通过RAFT聚合法制备了两嵌段聚合物PEGMA-b-PCL。将其自组装为胶束用作纳米药物载体,并以姜黄素(Cur)为胶束负载药物。考察了两嵌段聚合物结构、分子量及分布,表征了胶束载体粒径、形貌,测试了胶束载体的载药和释药性能。结果表明,不同嵌段聚合物相对分子质量范围为478~7318,此类聚合物具有较低的临界胶束浓度(CMC),在常规条件下(pH=7.4)其范围为0.920~1.600 μg/mL。胶束载体粒径范围为:68.34~186.30 nm。当n(CDPA)∶n(ε-CL)=1∶200时,胶束载药量和包封率最高,可达12.05%和75.26%。在不同pH值环境下,药物缓释性能可达15 d,其中pH=5.0时释药量可达35.38%。

    Abstract:

    ε-caprolactone(ε-CL), polyethylene glycol methyl ether methacrylate (PEGMA), and 4-cyano-4-(dodecylsulfanylthiocarbonyl)sulfanylpentanoic acid (CDPA) were respectively considered to be hydrophobic chain segment, hydrophilic chain segment, and initiator in the polymerization reaction. A bi-block polymer PEGMA-b-PCL was prepared by reversible addition-fragmentation chain transfer(RAFT)polymerization and the polymer were self-assembled into polymeric micelle as nanocarriers. The results showed that the relative molecular weight of the polymer was in the range of 478-7318, and the size distribution of the micelles was 68.34-186.30 nm. The polymeric micelle critical micelle concentration (CMC) (pH=7.4, 0.920 μg/mL~1.600 μg/m L) is lower. When n (CDPA): n(ε-CL) = 1: 200, the drug loading capacity and encapsulation efficiency of drug curcumin(Cur)loaded micelles are the as high as 12.05% and 75.26%, respectively. Under different conditions, the drug sustained release behaviour can be carried?out within 15 days, and the cumulative release amount of the drug can reach as high as 35.38% in the aqueous solution (pH=5.0).

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周国永,尹付琳,尹城武,王钰杰,陈雨鑫,刘超,成琳,杜海军.低临界胶束浓度PEGMA-b-PCL的制备及其 药物缓释性能[J].精细化工,2024,41(6):

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  • 收稿日期:2023-05-21
  • 最后修改日期:2023-08-27
  • 录用日期:2023-08-10
  • 在线发布日期: 2024-06-11
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