Drug, targeting ligand, and imaging agent are the three essential components in a nanoparticle-based drug delivery system. However, tremendous batch-to-batch variation of composition and drug content typically accompany the current approaches of building these components together. Herein, we report the design of photoactivatable platinum(IV) (Pt(IV)) amphiphiles containing one or two hydrophilic lactose targeting ligands per hydrophobic Pt(IV) prodrug for an all-in-one precise nanomedicine. Self-assembly of these Pt(IV) amphiphiles results in either micelle or vesicle formation with a fixed Pt/targeting moiety ratio and a constantly high content of Pt. The micelles and vesicles are capable of hepatoma cell-targeting, fluorescence/Pt-based CT imaging and have shown effective anticancer efficacy under laser irradiation in vitro and in vivo. This photoactivatable, active self-targeting, and multimodal theranostic amphiphile strategy shows great potential in constructing precise nanomedicine.

中文翻译：

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定制铂（IV）两亲物作为自靶向多合一组件，作为精确的多峰治疗药物纳米药物

药物，靶向配体和成像剂是基于纳米颗粒的药物递送系统中的三个基本组成部分。然而，组成和药物含量的批次间差异很大，通常伴随着将这些成分一起构建的当前方法。在这里，我们报告设计的光活化铂（IV）（Pt（IV））两亲物，每个疏水性Pt（IV）前药包含一个或两个亲水性乳糖靶向配体，用于多合一精确纳米医学。这些Pt（IV）两亲物的自组装会导致胶束或囊泡形成，并具有固定的Pt /靶向部分比率和恒定的Pt含量。胶束和囊泡能够靶向肝癌细胞，基于荧光/铂的CT成像，并在激光照射下显示出有效的抗癌功效体外和体内。这种可光活化，主动自我靶向和多模式治疗动物两亲策略显示出在构建精确的纳米药物方面的巨大潜力。