Triphenylphosphine-docetaxel conjugate-incorporated albumin nanoparticles for cancer treatment

Author:

Battogtokh Gantumur1,Gotov Oyuntuya1,Kang Jee He1,Cho Jinsung1,Jeong Tae Ho1,Chimed Ganzorig2,Ko Young Tag1

Affiliation:

1. College of Pharmacy & Gachon Institute of Pharmaceutical Sciences Gachon University, Incheon 406–799, South Korea

2. New Mongol Institute of Technology, Ulaanbaatar, Mongolia

Abstract

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.

Publisher

Future Medicine Ltd

Subject

Development,General Materials Science,Biomedical Engineering,Medicine (miscellaneous),Bioengineering

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