Li H, Li X, Wang Y, Ji J
MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
Mater Today Bio. 2019 Oct 25;4:100034. doi: 10.1016/j.mtbio.2019.100034. eCollection 2019 Sep.
To overcome the dilemma between passive tissue targeting and active cell targeting, nanomaterials are often required to exhibit the transition from 'stealth' to 'active targetable' in response to the pathological microenvironment. Here, we introduced a ternary surface modification method that incorporating active targeting ligand lactobionic acid with pH-sensitive mixed-charge surface. The resulted mixed-charge gold nanoparticles (LA@MC-GNPs) showed resistance to non-specific adsorption of proteins and uptake by HepG2 cells at normal tissue pH 7.4, while they underwent pH-sensitive aggregation and recovered active targeting capability at tumor acidic pH 6.5. The ternary surface modification method provided a simplest strategy to solve the dilemma between passive and active targeting of nanomedicine.
为了克服被动组织靶向和主动细胞靶向之间的困境，通常要求纳米材料能够响应病理微环境，从“隐身”状态转变为“主动可靶向”状态。在此，我们引入了一种三元表面修饰方法，即将活性靶向配体乳糖酸与pH敏感的混合电荷表面相结合。所得到的混合电荷金纳米颗粒（LA@MC-GNPs）在正常组织pH 7.4时对蛋白质的非特异性吸附和被HepG2细胞摄取具有抗性，而在肿瘤酸性pH 6.5时它们会发生pH敏感聚集并恢复活性靶向能力。这种三元表面修饰方法为解决纳米药物被动靶向和主动靶向之间的困境提供了一种最简单的策略。
