阿霉素温度/pH双敏型自组装嵌段共聚物胶束的制备

被引:22
作者
古建春
乔明曦
高玮
赵秀丽
胡海洋
徐佳
晋运环
陈大为
机构
[1] 沈阳药科大学药学院
关键词
阿霉素; 温度/pH敏感; 嵌段共聚物; 自组装胶束;
D O I
暂无
中图分类号
R943 [制剂学];
学科分类号
100702 [药剂学];
摘要
本文用透析法制备了新型温度/pH双敏自组装嵌段共聚物聚组氨酸-聚乳酸羟基乙酸-聚乙二醇-聚乳酸羟基乙酸-聚组氨酸(OLH-b-PLGA-b-PEG-b-PLGA-b-OLH)胶束,采用荧光探针技术测定其不同温度下临界胶束浓度(CMC);用透析法测定共聚物胶束的包封率和载药量;对胶束的粒径、形态和表面电位进行考察,并对阿霉素胶束的体外释药和pH敏感性进行了研究。CMC介于0.0224~0.0017μg.mL-1,胶束包封率为92.8%,载药量为15.7%;载药胶束粒径为(61.7±13.4)nm,zeta电位为-9.88 mV;阿霉素的体外释药速率随pH降低(pH 7.4~5.0)而增加。结果表明,胶束的CMC随温度升高而降低,体外释药具有明显的pH敏感性,该载体材料作为抗肿瘤药物的靶向传递系统具有较好的应用前景。
引用
收藏
页码:793 / 797
页数:5
相关论文
共 6 条
[1]
Super pH-sensitive multifunctional polymeric micelle for tumor pH e specific TAT exposure and multidrug resistance[J] Eun Seong Lee;Zhonggao Gao;Dongin Kim;Kyeongsoon Park;Ick Chan Kwon;You Han Bae Journal of Controlled Release 2008,
[2]
Injectable biodegradable temperature-responsive PLGA–PEG–PLGA copolymers: Synthesis and effect of copolymer composition on the drug release from the copolymer-based hydrogels[J] Mingxi Qiao;Dawei Chen;Xichen Ma;Yanjun Liu International Journal of Pharmaceutics 2005,
[3]
Biodegradable Triblock Copolymer of PLGA-PEG-PLGA Enhances Gene Transfection Efficiency[J] Ji Hoon Jeong;Sung Wan Kim;Tae Gwan Park Pharmaceutical Research 2004,
[4]
Sustained Intravesical Drug Delivery Using Thermosensitive Hydrogel[J] Pradeep Tyagi;Zhenhua Li;Michael Chancellor;William C. De Groat;Naoki Yoshimura;Leaf Huang Pharmaceutical Research 2004,
[5]
Poly( l -histidine)–PEG block copolymer micelles and pH-induced destabilization[J] Eun Seong Lee;Hyun Joon Shin;Kun Na;You Han Bae Journal of Controlled Release 2003,
[6]
Targetable HPMA copolymer-adriamycin conjugates. Recognition; internalization; and subcellular fate[J] Journal of Controlled Release 1998,