化学
体内
小干扰RNA
体外
转染
组合化学
癌细胞
基因传递
作者
Lin Zhu,Federico Perche,Tao Wang,Vladimir P. Torchilin
出处
期刊:Biomaterials
[Elsevier]
日期:2014-04-01
卷期号:35 (13): 4213-4222
被引量:178
标识
DOI:10.1016/j.biomaterials.2014.01.060
摘要
Co-delivery of hydrophilic siRNA and hydrophobic drugs is one of the major challenges for nanomaterial-based medicine. Here, we present a simple but multifunctional micellar platform constructed by a matrix metalloproteinase 2 (MMP2)-sensitive copolymer (PEG-pp-PEI-PE) via self-assembly for tumor-targeted siRNA and drug co-delivery. The micellar nanocarrier possesses several key features for siRNA and drug delivery, including (i) excellent stability; (ii) efficient siRNA condensation by PEI; (iii) hydrophobic drug solubilization in the lipid "core"; (iv) passive tumor targeting via the enhanced permeability and retention (EPR) effect; (v) tumor targeting triggered by the up-regulated tumoral MMP2; and (vi) enhanced cell internalization after MMP2-activated exposure of the previously hidden PEI. These cooperative functions ensure the improved tumor targetability, enhanced tumor cell internalization, and synergistic antitumor activity of co-loaded siRNA and drug.
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