Enhanced Apoptosis and Mitochondrial Cell Death by Paclitaxel-Loaded TPP-TPGS ₁₀₀₀ -Functionalized Nanoemulsion

Abstract

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.

Synchronized Codelivery of Combination Chemotherapies Intratumorally Using a Lipidic Lyotropic Liquid Crystal System

“…Cell toxicity was measured using the MTT assay, and cell cycle analysis was conducted using flow cytometry, following the previously reported protocols with slight modifications (described in the Supporting Information). , The total chemotherapeutic dose was fixed at 1 μM for all combinations of PTX and DOX treatments. The cytotoxicity results were analyzed using the median-effect model designed by Chou and Talalay. − …”