Paclitaxel Lipid Nanoparticles from Paclitaxel Prodrug Conjugates for the Treatment of Breast Cancer

Andrea Sacchetti – PhD, Erasmus MC; Christoph Stingl – PhD, Erasmus MC; Tarun Ojha – Postdoc, Erasmus MC; Yu Cai – PhD student, Erasmus MC; Timo ten Hagen – associate professor, Erasmus MC; Mohamadreza Amin – Pharm D. PhD., Erasmus MC

Introduction:

Paclitaxel (PTX) is a broad-spectrum anticancer drug used to treat breast, ovarian, lung, and other cancers by disrupting microtubule dynamics and blocking mitosis. [1] However, poor water solubility (~0.03 mg/mL) and inability to form salts have limited formulation options. [2][3] Existing PTX formulations (e.g., Taxol®, Genexol-PM®, Lipusu®, and Abraxane®) suffer from premature drug release, systemic toxicity, or high manufacturing cost. [4] To address these issues, we designed lipophilic PTX prodrug conjugates enabling stable formation of lipid nanoparticles, reducing premature drug leakage and improving stability at a lower cost.