Qi Junyang, Xiong Yue, Cheng Ke, Huang Qi, Cao Jingxiu, He Fumei, Mei Lin, Liu Gan, Deng Wenbin
School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University, Shenzhen 518107, China.
Department of Chemistry, City University of Hong Kong, Hong Kong, China.
Asian J Pharm Sci. 2021 Mar;16(2):222-235. doi: 10.1016/j.ajps.2020.09.001. Epub 2020 Oct 18.
Black phosphorus (BP) nano-materials, especially BP quantum dots (BPQDs), performs outstanding photothermal antitumor effects, excellent biocompatibility and biodegradability. However, there are several challenges to overcome before offering real benefits, such as poor stability, poor dispersibility as well as difficulty in tailoring other functions. Here, a "three-in-one" mitochondria-targeted BP nano-platform, called as BPQD-PEG-TPP, was designed. In this nano-platform, BPQDs were covalently grafted with a heterobifunctional PEG, in which one end was an aryl diazo group capable of reacting with BPQDs to form a covalent bond and the other end was a mitochondria-targeted triphenylphosphine (TPP) group. In addition to its excellent near-infrared photothermal properties, BPQD-PEG-TPP had much enhanced stability and dispersibility under physiological conditions, efficient mitochondria targeting and promoted ROS production through a photothermal effect. Both experiments demonstrated that BPQD-PEG-TPP performed much superior photothermal cytotoxicity than BPQDs and BPQD-PEG as the mitochondria targeted PTT. Thus this "three-in-one" nanoplatform fabricated through polymer grafting, with excellent stability, dispersibility and negligible side effects, might be a promising strategy for mitochondria-targeted photothermal cancer therapy.
黑磷（BP）纳米材料，尤其是BP量子点（BPQDs），具有出色的光热抗肿瘤效果、优异的生物相容性和生物降解性。然而，在带来实际益处之前，仍有几个挑战需要克服，比如稳定性差、分散性差以及难以定制其他功能。在此，设计了一种名为BPQD-PEG-TPP的“三合一”线粒体靶向BP纳米平台。在这个纳米平台中，BPQDs与一种异双功能PEG共价接枝，其中一端是能够与BPQDs反应形成共价键的芳基重氮基团，另一端是线粒体靶向三苯基膦（TPP）基团。除了具有出色的近红外光热性能外，BPQD-PEG-TPP在生理条件下具有大大增强的稳定性和分散性、高效的线粒体靶向性，并通过光热效应促进活性氧生成。两项实验均表明，作为线粒体靶向光热疗法，BPQD-PEG-TPP的光热细胞毒性比BPQDs和BPQD-PEG优越得多。因此，这种通过聚合物接枝制备的“三合一”纳米平台，具有出色的稳定性、分散性和可忽略不计的副作用，可能是线粒体靶向光热癌症治疗的一种有前景的策略。
