Triphenylphosphine-docetaxel conjugate-incorporated albumin nanoparticles for cancer treatment.

Aim: The objective of this study was to develop a mitochondria-targeted anticancer drug, docetaxel (DTX), for chemotherapy.

Materials & Methods: The DTX was conjugated to 4-carboxybutyl triphenylphosphonium (TPP) to enhance mitochondrial targeting, and the TPP-DTX conjugate was further loaded into folate-cholesteryl albumin (FA-chol-BSA) nanoparticles (NPs) to improve its biocompatibility.

Results & Conclusion: In vitro studies showed that TPP-DTX and its NP primarily accumulated in the mitochondria; generated high reactive oxygen species, leading to mitochondrial disruption and cell apoptosis; and had a higher cytotoxicity against cancer cells. In vivo antitumor studies indicated that the NP significantly suppressed tumor growth compared with free drugs in xenograft tumor-bearing mice. Our results demonstrated that TPP-DTX@FA-chol-BSA NPs could be a promising mitochondria-targeted anticancer prodrug for chemotherapy.