基于聚合物的肿瘤靶向载药体系.ppt

Southeast University 基于大分子的 药物控释 肿瘤靶向 Polymeric Tumor-Targeting Drug Controlled Release Du Yawei Drug Load 装载 定位 Targeting Drug Release 释放 胶束 Micelles 树枝状聚合物 Dendrimers Liposomes 微脂囊 聚合物-药物 偶联物 Polymer-drug conjugates Drug Load 装载 定位 主动 active 被动 passive Targeting 配合基-受体 Ligand-receptor EPR效应 EPR Effect 叶酸 多肽 正常组织 癌变部位 Drug Release 释放 pH 温度 降解 磁场 UV 电场 内因 外因 PDEAEMA PNIPAM -s-s- hydrazone bonds 多层 分子设计 Molecular Design 嵌段 分子量 端基 ATRP RAFT 点击化学 超分子 星形 开环 Cancer Drug Delivery：A CAPIR Cascade Circulation Accumulation Penetration Internalization Release Drug Retention Stealthy ~100 nm PEGylation Shield FG Neutral Stable Diffusivity 20nm Stable Neural Sticky to cell Cationic charge Expose FG Stable Release Cleavable Dissembling Size Surface Stability Tumor-Targeting, pH-Responsive, and Stable Unimolecular Micelles as Drug Nanocarriers for Targeted Cancer Therapy Xiaoqiang Yang, Jamison J. Grailer, Srikanth Pilla PEG-SS-PPS: Reduction-Sensitive Disulfide Block Copolymer Vesicles for Intracellular Drug Delivery Xiang Lan Wu, Jong Ho Kim Q. Sun et al. / Journal of Controlled Release 164 (2012) 156–169 Angew. Chem. Int. Ed. 2007, 46, 4999 –5002 Bioorg. Med. Chem. Lett. 25 (2015) 188–191 Chemistry–An Asian Journal 10 (2015) 1232-1238 International Journal of Pharmaceutics 493 (2015) 460–465 Q. Sun et al. Journal of Controlled Release 164 (2012) 156–169 Bioconjugate Chem. 2012, 23, 1322?1332 Bioconjugate Chem. 2012, 23, 1322?1332 Angew. Chem. Int. Ed. 2015, 54, 1–6 Confocal images of live HeLa cells. (a) No probe. (b) Treated with 20 uM of RhoSS. (c) Treated with 20 uM of RhoCC. (d) Preincubated with 100 uM of NEM and treated with 20 uM of RhoSS. (e) Unwashed cells treated with 40 uM of RhoSS. Structure of RhoSS and RhoCC. (a) Mechanism of unmasking for RhoSS. (b) Structures of RhoSS and control compound RhoCC. Org. Lett., Vol. 10, No. 5, 2008 J. Am. Chem. Soc. 2014, 136, 3579?3588 Absorption and emission changes of (A, C) activatable prodrug DCM-S-CPT (1