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 ([email protected]) 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难题，响应于病理学微环境，通常需要纳米材料表现出从“隐身”到“主动可靶向”的转变。在这里，我们介绍了一种三元表面改性方法，该方法将具有活性的靶向配体乳糖酸与pH敏感的混合电荷表面结合在一起。所得的混合电荷金纳米颗粒（[受电子邮件保护]）在正常组织pH 7.4时显示出对蛋白质非特异性吸附和HepG2细胞摄取的抵抗力，而它们在pH值为6.5的情况下经历了pH敏感的聚集和恢复的主动靶向能力。 。三元表面改性方法提供了最简单的策略来解决纳米药物被动和主动靶向之间的难题。