Nanomedicine: Enhancement of Chemotherapeutical Efficacy of Docetaxel by Using a Biodegradable Nanoparticle Formulation

The clinical dosage formulation of Paclitaxel and Docetaxel, Taxol® and Taxotere®, while having high efficacy, can cause serious side effects due to the adjuvant used. We have developed a system of nanoparticles (NPs) of biodegradable copolymer, poly(lactic acid)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLA-TPGS), for Docetaxel formulation to achieve enhanced, sustainable and controlled chemotherapeutic effectiveness and reduce the undesirable side actions. Docetaxel-loaded PLA-TPGS NPs were synthesized with desired size and physicochemical and pharmaceutical properties. In vitro studies using MCF-7 cancer cells have demonstrated the higher cellular uptake and therapeutic effects of the NP formulation. In vivo pharmacokinetics and biodistribution analysis have shown that one dose of the NP formulation of Docetaxel can achieve a 360-h effective chemotherapy with 3.44-fold higher therapeutic effect and 4.42-fold lower side effect than that of Taxotere® at the same dose of 10 mg/kg, as indicated by the larger area-under-the-curve and better biodistribution.