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纸质出版日期:2011-8-20,
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郑晓明, 蒋涛, 贺枫. PNIPAM-b-聚碳酸酯温敏胶束的制备及用作药物控制释放载体的研究[J]. 高分子学报, 2011,(8):895-902.
ZHENG Xiao-Ming, JIANG Tao, HE Feng. SYNTHESIS AND CHARACTERIZATION OF PNIPAM-b-POLYCARBONATE COPOLYMERS AS SELF-ASSEMBLED THERMOSENSITIVE MICELLES FOR DRUG DELIVERY[J]. Acta Polymerica Sinica, 2011,(8):895-902.
郑晓明, 蒋涛, 贺枫. PNIPAM-b-聚碳酸酯温敏胶束的制备及用作药物控制释放载体的研究[J]. 高分子学报, 2011,(8):895-902. DOI: 10.3724/SP.J.1105.2011.11120.
ZHENG Xiao-Ming, JIANG Tao, HE Feng. SYNTHESIS AND CHARACTERIZATION OF PNIPAM-b-POLYCARBONATE COPOLYMERS AS SELF-ASSEMBLED THERMOSENSITIVE MICELLES FOR DRUG DELIVERY[J]. Acta Polymerica Sinica, 2011,(8):895-902. DOI: 10.3724/SP.J.1105.2011.11120.
以多孔硅球固定化猪胰脂肪酶(IPPL)为催化剂
温敏性HO-PNIPAM为大分子引发剂
5-甲基-5-烯丙氧羰基-三亚甲基碳酸酯(MAC)和5
5-二甲基三亚甲基碳酸酯(DTC)为共聚单体
通过开环聚合合成了不同结构比例的两亲性嵌段型共聚物P(MAC-co-DTC)-b-PNIPAM.该嵌段型共聚物在水中可自组装形成稳定的胶束
其CMC值为20~60 mg/L
干态粒径20~70 nm
LCST值为38~43℃
细胞毒性实验显示其具有良好的生物相容性.以疏水性药物醋酸泼尼松为模型药物
研究了嵌段型共聚物胶束对药物的负载及释放行为
结果表明载药胶束具有良好的温敏性药物释放性能.
A series of poly(N-isopropylacrylamide) (PNIPAM)-blocked polycarbonates
P(MAC-co-DTC)-b-PNIPAM
were designed as thermosensitive micelles for drug delivery.The amphiphilic block copolymers were synthesized by enzymatic ring-opening copolymerization of HO-PNIPAM
5-methyl-5-allyloxycarbonyl-trimethylene carbonate (MAC) and 5
5-dimethyltrimethylene carbonate (DTC).The novel block copolymers were characterized by1H-NMR and GPC-MALLS analyses.All the amphiphilic copolymers were able to self-assemble into nano-sized micelles in aqueous solutions with hydrophilic PNIPAM shells and hydrophobic polycarbonates cores.The critical micelle concentration (CMC) determined by fluorescence spectroscopy using pyrene as a probe was around 20~60 mg/L.Transmission electron microscopy (TEM) measurements showed that the micelles presented even spherical shape and the diameters of them were about 20~70 nm.The micelles exhibited thermosensitivity at lower critical solution temperature (LCST) of around 38~43℃
which was related to the hydrophilic PNIPAM blocks.In vitro experiments demonstrated that the P(MAC-co-DTC)- b -PNIPAM showed low cytotoxicity.Furthermore
the micelles were loaded with hydrophobic drug of prednisone acetate (PA) and in vitro drug release investigation also displayed thermosensitivity.The results suggested that P(MAC-co-DTC)-b-PNIPAM copolymers would be a promising thermosensitive carrier for drug delivery.
嵌段型两亲性温敏胶束PNIPAM生物可降解聚碳酸酯酶促聚合药物控制释放毒性
Amphiphilic thermosensitive micellesPNIPAMBiodegradable polycarbonatesEnzymatic polymerizationDrug deliveryCytotoxicity
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