Advances in the formulations of non-injection administration of docetaxel

• Published in: Journal of drug targeting 2014-02, Vol.22 (2), p.87-94
• Main Authors: Zhang, Haiqun, Dou, Jinfeng, Zhai, Yingjie, Liu, Anchang, Zhai, Guangxi
• Format: Article
• Language: English
• Subjects: Animals; Chemistry, Pharmaceutical - methods; Docetaxel; Drug Administration Routes; Drug Delivery Systems - methods; Humans; liposomes; nanoparticles; non-injection administration; Solubility; Taxoids - administration & dosage; Taxoids - chemistry
• ISSN: 1061-186X; 1029-2330
• DOI: 10.3109/1061186X.2013.839686

Abstract Docetaxel is one of the most important anti-tumor drugs and has shown powerful therapeutic activity against breast cancer, non-small cell lung cancer, prostate cancer and so on. Owing to its poor water solubility and the efflux by P-glycoprotein (P-gp) and metabolism by CYP3A4 enzymes, it is generally administered as an injection form, the only manner for the current clinical application. However, the injection bearing polysorbate 80 and ethanol may cause adverse events such as severe hypersensitivity reactions, neutropenia, neurotoxicity, musculoskeletal toxicity and cumulative fluid retention, these adverse events limit clinical application and commercialization of docetaxel. Recently, various kinds of non-injection delivery systems for docetaxel have been developed to eliminate the polysorbate 80-based vehicle and increase the drug solubility. In this review, the non-injection delivery formulations of docetaxel for oral route, transdermal delivery, lung and rectal administration were discussed for future study and clinical application.