线粒体特殊的双层结构是癌症、代谢性疾病等疾病诊断和治疗中很有前景的治疗靶点。可以开发纳米载体，例如用亲线粒体部分修饰的脂质体，以将治疗分子发送到线粒体。本研究合成了DSPE-PEG-TPP聚合物缀合物，并用于制备线粒体靶向脂质体（TPPL），以提高化疗药物在线粒体中发挥作用的治疗指数并减少其副作用。制备了负载阿霉素 (Dox) 的 TPPL 和非靶向聚乙二醇化脂质体 (PPL)，并根据理化性质、形态、释放曲线、细胞摄取、线粒体定位和抗癌作用进行比较。所有制剂均为球形，具有适当的尺寸、分散性和 zeta 电位。脂质体在 4°C 下两个月的稳定性良好。 TPPL 定位于线粒体，而 PPL 则不然。空的TPPL和PPL对HCT116细胞没有细胞毒性。负载 Dox 的脂质体的释放动力学表明，TPPL 中释放的 Dox 在 pH 5.6 时比在 pH 7.4 时更高，这表明释放的药物在肿瘤环境中的积累更高。由于药物持续释放，负载 Dox 的 TPPL 和 PPL 的半最大抑制浓度分别比游离 Dox 低 1.62 倍和 1.17 倍。当 HCT116 细胞用负载 Dox 的 TPPL 处理时，活性氧水平显着增加。总之，TPPL 可能是有前途的将药物递送至肿瘤线粒体的载体。

The special bilayer structure of mitochondrion is a promising therapeutic target in the diagnosis and treatment of diseases such as cancer and metabolic diseases. Nanocarriers such as liposomes modified with mitochondriotropic moieties can be developed to send therapeutic molecules to mitochondria. In this study, DSPE-PEG-TPP polymer conjugate was synthesized and used to prepare mitochondria-targeted liposomes (TPPLs) to improve the therapeutic index of chemotherapeutic agents functioning in mitochondria and reduce their side effects. Doxorubicin (Dox) loaded-TPPL and non-targeted PEGylated liposomes (PPLs) were prepared and compared based on physicochemical properties, morphology, release profile, cellular uptake, mitochondrial localization, and anticancer effects. All formulations were spherically shaped with appropriate size, dispersity, and zeta potential. The stability of the liposomes was favorable for two months at 4 °C. TPPLs localize to mitochondria, whereas PPLs do not. The empty TPPLs and PPLs were not cytotoxic to HCT116 cells. The release kinetics of Dox-loaded liposomes showed that Dox released from TPPLs was higher at pH 5.6 than at pH 7.4, which indicates a higher accumulation of the released drug in the tumor environment. The half-maximal inhibitory concentration of Dox-loaded TPPLs and PPLs was 1.62-fold and 1.17-fold lower than that of free Dox due to sustained drug release, respectively. The reactive oxygen species level was significantly increased when HCT116 cells were treated with Dox-loaded TPPLs. In conclusion, TPPLs may be promising carriers for targeted drug delivery to tumor mitochondria.