State Key Laboratory of Natural Medicines, Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
State Key Laboratory of Natural Medicines, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Mater Sci Eng C Mater Biol Appl. 2015 Nov 1;56:280-5. doi: 10.1016/j.msec.2015.06.034. Epub 2015 Jun 20.
A new cationic polymer eprosartan-graft-PEI (ESP) containing eprosartan (ES) and polyethylenimine 1.8K was successfully developed and employed as a safe gene vector to assemble a drug (ES) and gene co-delivery complex (ESP/pDNA). Chondroitin sulfate (CS) was then used as a coating polymer to shield the surface charge of ESP/pDNA complexes, as well as a tumor targeting entity to ensure specific delivery of CS/ESP/pDNA complexes. The CS/ESP/pDNA complexes with desirable particle size and zeta potential, exhibited amidase-responsive drug release and CS-mediated endocytosis in vitro. As compared with ESP/pDNA complexes, in vivo imaging results demonstrated decreased reticuloendothelial system uptake and remarkably increased tumor accumulation of CS/ESP/pDNA complexes. All these findings indicated the potential of CS/ESP/pDNA as a promising tumor-targeted drug and gene co-delivery system.
一种新型阳离子聚合物依普罗沙坦接枝聚乙亚胺（ESP）被成功开发并用作安全的基因载体，用于组装药物（ES）和基因共递药复合物（ESP/pDNA）。然后，硫酸软骨素（CS）被用作涂层聚合物来屏蔽 ESP/pDNA 复合物的表面电荷，同时作为肿瘤靶向实体以确保 CS/ESP/pDNA 复合物的特异性递送。具有理想粒径和 ζ 电位的 CS/ESP/pDNA 复合物表现出酰胺酶响应性药物释放和 CS 介导的细胞内吞作用。与 ESP/pDNA 复合物相比，体内成像结果表明，CS/ESP/pDNA 复合物的网状内皮系统摄取减少，肿瘤积累显著增加。所有这些发现表明 CS/ESP/pDNA 作为一种有前途的肿瘤靶向药物和基因共递药系统的潜力。
