穿膜肽R8和pH敏感型可断裂PEG共修饰脂质体的构建.pdf

See discussions, stats, and author profiles for this publication at: /publication/282739586 The construction of cell-penetrating peptide R8 and pH sensitive cleavable polyethylene glycols co-modified liposomes Article June 2015 CITATION READS 1 69 4 authors, including: Li Zhang Huile Gao National University of Singapore Sichuan University 17 PUBLICATIONS 166 CITATIONS 128 PUBLICATIONS 2 203 CITATIONS SEE PROFILE SEE PROFILE Some of the authors of this publication are also working on these related projects: Tumor microenvironment sensitive nanoparticles View project Carbonaceous dots for bioimaging and drug delivery View project All content following this page was uploaded by Huile Gao on 11 December 2015. The user has requested enhancement of the downloaded file. 760 药学学报 Acta Pharmaceutica Sinica 20 15, 50 (6): 760 766 膜肽R8 和pH 敏感型可断裂PEG 共修饰脂质体的构建 莉, 王 蛘, 高会乐, 何 勤* ( 四川大学华西药学院, 靶向药物与传递系统教育部重点实验室, 四川 成都 610041) 摘要: 本文旨在构建穿膜肽R8 (RRRRRRRR) 和pH 敏感型PEG ( 聚乙二醇, polyethylene glycols) 共修饰的 脂质体 (R8 peptide and pH sensitive PEG co-modified liposomes, Cl-Lip) 用于乳腺癌的靶向药物传递。通过卵磷 脂、胆固醇、DSPE-PEG2K-R8 和PEG5K-Hz-PE (pH 敏感型PEG) 为材料制备共修饰脂质体, 对其粒径和zeta 电 位进行表征。采用4T1 细胞考察不同预孵育条件下细胞对Cl-Lip 的摄取。同时对其入胞 径、溶酶体逃逸能力 及肿瘤球穿透能力进行考察。结果表明, Cl-Lip 粒径为 ( 110.4 ±5.2) nm, PDI 为0.207 ±0.039, zeta 电位为 ( 3.46 ± 0.05) mV 。体外实验证明, Cl-Lip 具有良好的血清稳定性。在不同的预孵育时间点, 4T1 细胞对Cl-Lip 的摄