文献：Biotin-conjugated PEGylated porphyrin self-assembled nanoparticles co-targeting mitochondria and lysosomes for advanced chemo-photodynamic combination therapy†

作者：Baskaran Purushothaman , Jinhyeok Choi , Solji Park , Jeongmin Lee , Annie Agnes Suganya Samson , Sera Hong and Joon Myong Song

文献链接：https://pubs.rsc.org/en/content/articlehtml/2018/tb/c8tb01923a

 In this study, biotin-conjugated PEGylated photosensitizer (PS) self-assembled nanoparticles (meso-tetraphenylporphyrin (TPP)–PEG–biotin SANs) were prepared via a self-assembly process to serve as nanocarriers for chemo-drugs as well as PSs. Electron microscopy results reveal the spherical shape of the nanoparticles (NPs). In the NPs, conjugated biotin plays a key role in selective tumor targeting. In vitro cellular experiments revealed the rapid cellular uptake of the TPP–PEG–biotin conjugates by MCF-7 cells that overexpress the biotin receptor, and verified that the conjugates were much more effective PSs than TPPS used as control in the cytotoxicity test. Interestingly, subcellular localization studies showed that the conjugates and their self-assembled NPs were localized mainly in mitochondria and partially in lysosomes, whereas TPPS was localized only in lysosomes. With the exclusive localization in mitochondria, high-content cell based assay showed that the TPP–PEG–biotin SANs induced rapid mitochondrial membrane potential transition (MPT), leading to cellular apoptosis. The chemo-drug doxorubicin (DOX) was successfully encapsulated in the TPP–PEG–biotin SANs (DOX@TPP–PEG–biotin) and had synergistic effects with enhanced cytotoxicity after PDT action. 

在这项研究中，通过自组装过程制备了生物素偶联的聚乙二醇化光敏剂（PS）自组装纳米粒子（meso-四苯基卟啉（TPP）-PEG-生物素-SAN），作为化学药物和PS的纳米载体。

电子显微镜结果显示了纳米粒子（NP）的球形。在NP中，共轭生物素在选择性肿瘤靶向中起着关键作用。体外细胞实验揭示了过度表达生物素受体的MCF-7细胞对TPP-PEG-生物素偶联物的快速细胞摄取，并验证了偶联物比用作细胞毒性试验对照的TPPS更有效。

亚细胞定位研究表明，偶联物及其自组装NP主要定位在线粒体中，部分定位在溶酶体中，而TPPS仅定位在溶酶体。高含量细胞检测表明，TPP-PEG-生物素SANs仅在线粒体中定位，可诱导线粒体膜电位快速转换（MPT），导致细胞凋亡。

化疗药物阿霉素（DOX）成功封装在TPP-PEG-生物素SAN中(DOX@TPP-PEG-生物素），并在PDT作用后具有增强细胞毒性的协同作用。

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