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1.四川大学高分子科学与工程学院 成都 610065
2.高分子材料工程国家重点实验室(四川大学) 成都 610065
陈元维,E-mail:chenyuanweizm@163.com Yuan-wei Chen, E-mail:chenyuanweizm@163.com
罗祥林,E-mail:luoxl_scu@126.com Xiang-lin Luo, E-mail:luoxl_scu@126.com
纸质出版日期:2016-10,
收稿日期:2016-2-3,
修回日期:2016-2-3,
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陆爱菁, 侯宇, 吴正中, 陈元维, 罗祥林. 双重敏感的磺酸甜菜碱-姜黄素药物载体的合成和表征[J]. 高分子学报, 2016,(10):1400-1408.
Lu Ai-jing, Hou Yu, Wu Zheng-zhong, Chen Yuan-wei, Luo Xiang-lin. Synthesis and Characterization of a Dual-sensitive Copolymer Containing Curcumins and Zwitterionic Sulfobetaines as Drug Delivery Carrier[J]. Acta Polymerica Sinica, 2016,(10):1400-1408.
陆爱菁, 侯宇, 吴正中, 陈元维, 罗祥林. 双重敏感的磺酸甜菜碱-姜黄素药物载体的合成和表征[J]. 高分子学报, 2016,(10):1400-1408. DOI: 10.11777/j.issn1000-3304.2016.16047.
Lu Ai-jing, Hou Yu, Wu Zheng-zhong, Chen Yuan-wei, Luo Xiang-lin. Synthesis and Characterization of a Dual-sensitive Copolymer Containing Curcumins and Zwitterionic Sulfobetaines as Drug Delivery Carrier[J]. Acta Polymerica Sinica, 2016,(10):1400-1408. DOI: 10.11777/j.issn1000-3304.2016.16047.
合成了聚姜黄素-二硫键-聚甲基丙烯酸二乙胺基乙酯-聚磺酸甜菜碱(Cur-DA-ss-PDEA-PS,或简写为Cur-ss-PDEA-PS),采用核磁、红外对聚合物结构进行了表征,用示差扫描量热法测试了聚合物热性能.用溶剂挥发法制备聚合物胶束,形成了聚磺酸甜菜碱为亲水壳层、聚姜黄素为疏水核、二硫键作为还原敏感基团和聚甲基丙烯酸二乙氨基乙酯为pH敏感基团的胶束.用荧光分光光度计测定了临界胶束浓度,动态光散射以及扫描电镜对胶束结构及性质进行了表征.结果显示,胶束稳定性良好,粒径分布较窄,且具有pH敏感性和还原敏感性.胶束载药量及包封率测试结果显示,相比于聚己内酯为内核的聚合物胶束,聚姜黄素的引入提高了胶束对药物的封装效果.
A copolymer poly(curcumin)-ss-
b
-poly(2-(diethylamino)ethylmethacrylate)-poly{
N
-[2-(methacryloyloxy)ethyl]-
N
N
-diethyl-
N
-(3-sulfopropyl)-ammonium} (Cur-DA-ssPDEA-PS) was synthesized with the combination of atom radical transfer polymerization (ATRP) and conjugation and by sulfonation.Molecular structure of the copolymer was confirmed by
1
H-NMR and FTIR.Thermophysical properties of the copolymer were determined by DSC.Cur-DA-ssPDEA-PS micelles were formed by solvent evaporation using poly(zwitterionic sulfobetaines) as hydrophilic shell
poly(curcumin) as hydrophobic core
and DEA as pH sensitive content and disulfide as redox responsive linkage.Critical micelle concentration (CMC) of the copolymer in water was estimated using pyrene as a hydrophobic fluorescence probe.Dynamic light scattering (DLS) measurement was performed to determine the micellar size and distribution.Micelle morphology was observed by scanning electron microscopy (SEM).CMC obtained was about 10
-3
mg/mL
revealing that the micelles were stable.The micelle diameters were all below 200 nm with a narrow size distribution.There existed a buffer platform in pH titration curve and the micelle sizes changed when pH varying from 7.4 to 5.0.pH responsivity of the micelles was confirmed by these results.When treated by 10 mmol/L glutathione (GSH)
the micelles were damaged and aggregated
indicating a reduced micelle responsivity.The higher drug loading than PCL-ss-PDEA-PS indicated improvement of hydrophobic drug encapsulation by introduction of curcumins.
pH/还原敏感的高分子胶束药物载体磺酸甜菜碱姜黄素
pH/Redox dual-sensitive copolymerMicellesDrug delivery carrierSulfobetainesCurcumin
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