This report focused on a novel nano-drug delivery system (GA-DTX-PVP/CuS-TSL) by combining glycyrrhetinic acid, copper sulfide nanoparticles, and docetaxel (DTX) with thermo-sensitive liposomes, which not only could achieve drug targeting distribution, but also could combine chemotherapy with phototherapy for tumor therapy. The particle size and DL of GA-DTX-PVP/CuS-TSL were 251.2 ± 0.40 nm (PDI = 0.15) and 7.51 ± 0.15%, respectively. The physicochemical properties, pharmacokinetics, biodistribution, and antitumor effects in vitro and in vivo of GA-DTX-PVP/CuS-TSL were also carried out. The result showed GA-DTX-PVP/CuS-TSL had obvious slower and temperature-dependent drug release effect when compared with DTX solution and DTX-PVP/CuS-TSL. In comparison to DTX solution group, the cell growth inhibition rates of DTX-PVP/CuS-TSL and GA-DTX-PVP/CuS-TSL groups on SMMC-7721 cells were significantly enhanced under the same conditions. Furthermore, when combined with 808 nm laser irradiation, the cell growth inhibition rates of DTX-PVP/CuS-TSL and GA-DTX-PVP/CuS-TSL groups were further enhanced. Moreover, GA-DTX-PVP /CuS-TSL could prolong the circulation time of DTX in vivo and improve the targeted distribution of DTX at the tumor sites of S₁₈₀ tumor-bearing mice. When combined with 808 nm of near-infrared light irradiation, GA-DTX-PVP/CuS-TSL had much more obvious anti-tumor activity both in vitro and in vivo than that of DTX solution and DTX-PVP/CuS-TSL. This study may provide certain theoretical basis for safe and effective treatment of tumor.

本报告重点介绍了一种通过将甘草次酸、硫化铜纳米颗粒和多西紫杉醇 (DTX) 与热敏脂质体相结合的新型纳米给药系统 (GA-DTX-PVP/CuS-TSL)，不仅可以实现药物靶向分布，但也可以结合化学疗法和光疗法进行肿瘤治疗。GA-DTX-PVP/CuS-TSL 的粒径和 DL 分别为 251.2 ± 0.40 nm (PDI = 0.15) 和 7.51 ± 0.15%。还进行了GA-DTX-PVP/CuS-TSL的理化性质、药代动力学、生物分布和体外和体内抗肿瘤作用。结果表明，与DTX溶液和DTX-PVP/CuS-TSL相比，GA-DTX-PVP/CuS-TSL具有明显的缓释和温度依赖性药物释放效应。与 DTX 解决方案组相比，DTX-PVP/CuS-TSL和GA-DTX-PVP/CuS-TSL组在相同条件下对SMMC-7721细胞的细胞生长抑制率显着增强。此外，当结合808 nm激光照射时，DTX-PVP/CuS-TSL和GA-DTX-PVP/CuS-TSL组的细胞生长抑制率进一步增强。此外，GA-DTX-PVP /CuS-TSL 可以延长 DTX 在体内的循环时间，提高 DTX 在 S 肿瘤部位的靶向分布。₁₈₀只荷瘤小鼠。GA-DTX-PVP/CuS-TSL结合808 nm近红外光照射，在体外和体内均比DTX溶液和DTX-PVP/CuS-TSL具有更明显的抗肿瘤活性。本研究可为肿瘤的安全有效治疗提供一定的理论依据。