光敏活性氧自由基响应脂质体的制备和评价

发布时间：2018-09-07 15:22

【摘要】：本文制备光敏感型活性氧自由基(reactive oxygen species,ROS)响应脂质体,研究其体外抗肿瘤活性。采用硫酸铵梯度法制备共输送光敏剂八丁氧基酞菁钯[1,4,8,11,15,18,22,25-octabutoxypalladium phthalocyanine,Pd PC(OBu)_8]与盐酸多柔比星(doxorubicin hydrochloride,DOX)的脂质体[liposome loaded with Pd PC(OBu)_8and DOX,LPD],考察LPD的粒径、zeta电位、透射电镜照片、光敏感型ROS响应药物的光响应释放及在血清中稳定性,进一步考察LPD在MCF-7细胞中的细胞毒性、细胞摄取及细胞内单线态氧(singlet oxygen,~1O_2)水平。结果显示,LPD的粒径为(169.3±1.2)nm,PDI为0.198±0.003,粒径均匀,zeta电位为(-39.8±0.8)m V。LPD具有良好的光响应释放特性,在730 nm激光以300 m W·cm~(-2)光照强度下,5 min内DOX释放率达到95.5%。LPD能显著促进DOX的细胞摄取,而且光照时细胞内能产生大量~1O_2。与游离DOX相比,LPD未光照时IC_(50)下降67.9%,光照时IC_(50)下降85.7%。因此,光敏ROS响应脂质体是具有前景的给药系统。
[Abstract]:In this paper, photo-sensitive reactive oxygen species (reactive oxygen species,ROS) -responsive liposomes were prepared to study their antitumor activity in vitro. The liposomes (liposome loaded with Pd PC (OBu) 8 and DOX,LPD) transporting Guang Min agent octabutoxypalladium phthalocyanine,Pd PC (OBu) 8 and doxorubicin hydrochloride (doxorubicin hydrochloride,DOX) were prepared by ammonium sulfate gradient method. The photo-responsive release of photo-sensitive ROS and its stability in serum were investigated to investigate the cytotoxicity, cellular uptake and intracellular monolinear oxygen (singlet oxygen,~1O_2) level of LPD in MCF-7 cells. The results showed that the particle size of LPD was (169.3 卤1.2) nm,PDI, 0.198 卤0.003, and the average particle size was (-39.8 卤0.8) m V.LPD. The DOX release rate within 5 min of 730 nm laser irradiation at 300MW cm~ (-2) could significantly promote the uptake of DOX cells. In addition, the cells can produce a large amount of 1 O 2 during illumination. Compared with free DOX, IC_ _ (50) decreased 67.9 and IC_ _ (50) decreased 85.7. Therefore, Guang Min ROS responsive liposome is a promising drug delivery system.
【作者单位】：第二军医大学药学院;
【基金】：国家自然科学基金资助项目(30801441,81773278) 军队后勤科研重大项目(AWS14J011)
【分类号】：R943

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