title: Nanomedicine: enhancement of chemotherapeutical efficacy of docetaxel by using a biodegradable nanoparticle formulation.
abstract: 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- -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 cellular uptake and lack of cytotoxicity 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.
authors.affiliation: Department of Chemical & Biomolecular Engineering, National University of Singapore, Singapore 117576, Singapore.
authors.forename: Chee Wee
authors.initials: CW
authors.lastname: Gan
authors.forename: Shu
authors.initials: S
authors.lastname: Chien
authors.forename: Si-Shen
authors.initials: SS
authors.lastname: Feng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D000077143:Docetaxel; D004357:Drug Synergism; D006801:Humans; D050997:Nanomedicine / Q000379:methods / Q000639:trends*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D043823:Taxoids / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D043823:Taxoids; D000077143:Docetaxel