Reconstituting Low-Density Lipoprotein with NIR-Absorbing Organic Photothermal Agents for Targeted Killing of Cancer Cells.

Photothermal therapy (PTT) systems typically do not possess intrinsic tumor-targeting capability, resulting in indiscriminate thermal damages to both cancer and normal cells. Herein, we report a low-density lipoprotein (LDL)-based nanosystem (denoted as MTTQ@LDL) for targeted photothermal killing of cancer cells. Such a nanosystem is fabricated by reconstituting the lipophilic core of LDL with an organic photothermal agent MTTQ. The reconstitution process improves the supramolecular photothermal effects of MTTQ assemblies, which contributes to the significantly enhanced photothermal conversion efficiency (41.3% versus 16.2%). MTTQ@LDL can actively target LDL receptor-overexpressed cancer cells via the receptor-mediated endocytosis, enabling the selective killing of cancer cells over normal cells (98% versus 7%) post NIR irradiation. Reconstituted LDL can serve as a promising platform for targeted delivery of functional materials, holding great promise in tumor eradication in vivo. This article is protected by copyright. All rights reserved.