Nanotheranostics with comprehensive diagnostic and therapeutic capabilities show exciting cancer treatment potentials. Here, we develop an excipient-free drug delivery system for cancer diagnosis as well as therapy, in which a near infra-red photosensitizer and a chemotherapeutic drug can be self-delivered without any carriers. The building block of the drug delivery system was synthesized by covalently conjugating four anticancer drugs (7-ethyl-10-hydroxy-camptothecin, SN-38) with a photosensitizer (porphyrin) via hydrolyzable ester linkage, which endows the drug delivery system with 100% active pharmaceutical ingredients, excellent imaging, and therapeutic functionalities. The conjugates can readily self-assemble into nanosheets (PS NSs) and remain stable for at least 20 days in aqueous solution. In PS NSs, fluorescence resonance energy transfer (FRET) dominates the fluorescence of SN-38 and enables to monitor the drug release fluorescently. The PS NSs also show excellent anticancer activity in vitro, due to the increased cell uptake with the synergistic effect of photodynamic therapy and chemotherapy.

中文翻译：

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不含赋形剂的卟啉/ SN-38纳米热学药物，用于药物递送和细胞成像

具有综合诊断和治疗能力的纳米疗法具有令人兴奋的癌症治疗潜力。在这里，我们开发了一种用于癌症诊断和治疗的无赋形剂给药系统，该系统无需任何载体即可自动递送近红外光敏剂和化学治疗药物。通过可水解酯键将四种抗癌药物（7-乙基-10-羟基喜树碱，SN-38）与光敏剂（卟啉）共价缀合，合成了药物传递系统的组成部分，使药物传递系统具有100种％活性药物成分，出色的成像和治疗功能。缀合物可以很容易地自组装成纳米片（PS NS），并在水溶液中保持稳定至少20天。在PS NS中，荧光共振能量转移（FRET）支配着SN-38的荧光，并能够监控药物的荧光释放。PS NSs还显示出出色的抗癌活性在体外，由于增加的细胞摄取与光动力疗法和化学疗法的协同作用。