Enhanced apoptosis and mitochondrial cell death by paclitaxel-loaded TPP-TPGS1000-functionalized nanoemulsion - supplementary data

Background: The present research was designed to develop a nanoemulsion (NE) of triphenylphosphine-

D-α-tocopheryl-polyethylene glycol succinate (TPP-TPGS1000) and paclitaxel (PTX) to effectively deliver

PTX to improve breast cancer therapy. Materials & methods: A quality-by-design approach was applied

for optimization and in vitro and in vivo characterization were performed. Results: The TPP-TPGS1000-

PTX-NE enhanced cellular uptake, mitochondrial membrane depolarization and G2M cell cycle arrest

compared with free-PTX treatment. In addition, pharmacokinetics, biodistribution and in vivo live

imaging studies in tumor-bearing mice showed that TPP-TPGS1000-PTX-NE had superior performance

compared with free-PTX treatment. Histological and survival investigations ascertained the nontoxicity

of the nanoformulation, suggesting new opportunities and potential to treat breast cancer. Conclusion:

TPP-TPGS1000-PTX-NE improved the efficacy of breast cancer treatment by enhancing its effectiveness and

decreasing drug toxicity.