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基于星型共聚物Ad-(PCL-b-PDEAEMA-b-PPEGMA)₄的pH敏感胶束用于药物控释

pH-Sensitive Micelles Based on Star Copolymer Ad-(PCL-b-PDEAEMA-b-PPEGMA)₄ for Controlled Drug Delivery.

作者信息

Yang Huiyan, Guo Jianwei, Tong Rui, Yang Chufen, Chen Jem-Kun

机构信息

School of Chemical Engineering & Light Industry, Guangdong University of Technology, Guangzhou 510006, China.

Department of Materials Science and Engineering, National Taiwan University of Science and Technology, No. 43, Sec. 4, Keelung Road, Taipei 106, Taiwan.

出版信息

Polymers (Basel). 2018 Apr 14;10(4):443. doi: 10.3390/polym10040443.

DOI:10.3390/polym10040443
PMID:30966478
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6415201/
Abstract

Enhancing drug loading efficacy and stability of polymeric micelles remains a grand challenge. Here we develop adamantane-based star copolymers adamantane-[poly(ε-caprolactone)--poly(2-(diethylamino)ethyl methacrylate)--poly(poly(ethylene glycol) methyl ether methacrylate)]₄ (Ad-(PCL--PDEAEMA--PPEGMA)₄) and their self-assembled micelles for controlled drug delivery. Results show that the polymers have excellent stability in solution with low critical micelle concentration (CMC) (0.0025⁻0.0034 mg/mL) and the apparent base dissociation constant (p) of the polymers is from 5.31 to 6.05. Dynamic light scattering analysis exhibits the great environmental response capability of the pH-sensitive micelles according to particle sizes and zeta potentials. With the synergy effect of the adamantane and hydrophobic block, the micelles display the high Doxorubicin (DOX) loading efficacy (up to 22.4%). The DOX release study shows that the micelles are capable of controlled release for drug. This work indicates the Ad-(PCL--PDEAEMA--PPEGMA)₄ micelles may provide new guidelines for drug control and release system in overcoming cancer treatment.

摘要

提高聚合物胶束的载药效率和稳定性仍然是一个巨大的挑战。在此，我们开发了基于金刚烷的星形共聚物金刚烷-[聚(ε-己内酯)-聚(甲基丙烯酸2-(二乙氨基)乙酯)-聚(聚乙二醇甲基醚甲基丙烯酸酯)]₄（Ad-(PCL-PDEAEMA-PPEGMA)₄）及其自组装胶束用于可控药物递送。结果表明，这些聚合物在溶液中具有优异的稳定性，临界胶束浓度（CMC）较低（0.0025⁻0.0034 mg/mL），聚合物的表观碱解离常数（p）为5.31至6.05。动态光散射分析根据粒径和zeta电位显示了pH敏感胶束具有很强的环境响应能力。由于金刚烷和疏水嵌段的协同作用，胶束表现出较高的阿霉素（DOX）载药效率（高达22.4%）。DOX释放研究表明，胶束能够实现药物的控释。这项工作表明，Ad-(PCL-PDEAEMA-PPEGMA)₄胶束可能为克服癌症治疗中的药物控制和释放系统提供新的指导。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/6c7bd9222f19/polymers-10-00443-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/df94b62ce558/polymers-10-00443-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/1a48d8bcd9a3/polymers-10-00443-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/e688daaa3307/polymers-10-00443-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/324e68969625/polymers-10-00443-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/04bb506327d4/polymers-10-00443-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/2ac40cdcbbf7/polymers-10-00443-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/ea0f687d3a92/polymers-10-00443-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/a65b231ff8f8/polymers-10-00443-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/6c7bd9222f19/polymers-10-00443-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/df94b62ce558/polymers-10-00443-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/1a48d8bcd9a3/polymers-10-00443-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/e688daaa3307/polymers-10-00443-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/324e68969625/polymers-10-00443-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/04bb506327d4/polymers-10-00443-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/2ac40cdcbbf7/polymers-10-00443-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/ea0f687d3a92/polymers-10-00443-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/a65b231ff8f8/polymers-10-00443-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd56/6415201/6c7bd9222f19/polymers-10-00443-g007.jpg

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