高载药诱导的聚2-噁唑啉胶束形态变化研究
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第二军医大学药学院,第二军医大学药学院,第二军医大学药学院

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国家“重大新药创制”专项(2013ZX09J13109-04B).


Study of morphological changes of poly(2-oxazoline) micelles induced by high loading of drugs
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Department of Pharmaceutical Science,College of Pharmacy,Second Military Medical University,Department of Pharmaceutical Science,College of Pharmacy,Second Military Medical University,Department of Pharmaceutical Science,College of Pharmacy,Second Military Medical University

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Supported by National Major Project for "Significant New Drug Development" (2013ZX09J13109-04B).

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    摘要:

    目的 制备载紫杉醇的聚2-噁唑啉纳米胶束,通过改变投药量考察药物引起的胶束形态变化,以期构建新型的高荷载嵌段共聚物胶束递药系统。方法 采用薄膜水化法制备聚2-噁唑啉载药胶束,以粒径、包封率和载药量等评价其理化性质,采用膜透析法考察其体外释药特性,利用CCK-8法测定其细胞毒性。结果 随着投药比由80∶100(紫杉醇与聚2-噁唑啉质量比)增加至110∶100,胶束逐渐由球形延长,变为蠕虫状。投药比为80∶100时,球形胶束的平均粒径为(43.17±0.95)nm,包封率为(88.81±2.93)%,载药量为(40.49±2.03)%;投药比增加至110∶100后,所得蠕虫状胶束的平均粒径为(107.83±1.51)nm,包封率为(77.08±0.97)%,载药量为(40.34±0.51)%。球形和蠕虫状胶束在磷酸盐缓冲液中24 h的累积释放量分别达到(76.58±3.07)%和(77.66±1.00)%,在含2%小牛血清白蛋白的PBS溶液中24 h的累积释放量高达(100.31±1.80)%和(99.73±2.56)%。球形胶束和蠕虫状胶束对人肺腺癌细胞A549的杀伤IC50值分别为0.336和0.342μg/mL。结论 成功制备了高荷载的球形和蠕虫状载药胶束,体外细胞毒性实验证明其具备抗肿瘤活性。

    Abstract:

    Objective To prepare the paclitaxel-loaded poly(2-oxazolyl) nano-micelles and to investigate the morphological changes of nano-micelles after changing drug dosage, so as to establish a novel block copolymer micelles delivery system with high loading capacity. Methods The paclitaxel-loaded poly(2-oxazolyl) nano-micelles were prepared using filming-rehydration method. The physical and chemical properties of the prepared nano-micelles, including particle size, encapsulation efficiency and drug loading efficiency, were characterized. The in vitro release characteristics of the prepared nano-micelles were investigated by membrane dialysis method, and the cytotoxicity was determined by CCK-8 method. Results The morphology of micelles gradually extended from spherical to worm-like when the mass ratio of paclitaxel and poly(2-oxazoline) increased from 80:100 to 110:100. The particle size, encapsulation efficiency and drug loading efficiency of spherical micelles were (43.17±0.95) nm, (88.81±2.93)% and (40.49±2.03)%, respectively, while those of worm-like micelles were (107.83±1.51) nm, (77.08±0.97)% and (40.34±0.51)%, respectively. The 24 h cumulative release rates of spherical micelles and worm-like micelles in PBS were (76.58±3.07)% and (77.66±1.00)%, respectively; meanwhile, those in PBS with 2% bovine serum albumin were up to (100.31±1.80)% and (99.73±2.56)%, respectively. The IC50 values of sphere micelles and worm-like micelles on human lung adenocarcinoma cell line A549 were 0.336 μg/mL and 0.342 μg/mL, respectively. Conclusion Paclitaxel-loaded spherical micelles and worm-like micelles with high loading capacity have been successfully prepared. In vitro cytotoxicity Results have found that both micelles have anti-tumor activities.

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  • 收稿日期:2016-10-10
  • 最后修改日期:2016-11-25
  • 录用日期:2017-01-09
  • 在线发布日期: 2017-02-27
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