The anticancer drug docetaxel (Taxotere) is formulated in the nonionic surfactant polysorbate 80 (Tween 80). Early in the clinical development of docetaxel, it became clear that docetaxel administration is associated with the occurrence of unpredictable (acute) hypersensitivity reactions and cumulative fluid retention. These side-effects have been attributed, in part, to the presence of polysorbate 80 and have consequently initiated research focused on the development of a less-toxic, better-tolerated polysorbate 80-free formulation of docetaxel. More recently, there is an increasing interest in developing a (polysorbate 80-free) docetaxel formulation that selectively targets malignant tissue, thereby increasing efficacy while decreasing the occurrence of side-effects related to wide and nonspecific body distribution. This review aims to discuss the preclinical and clinical results of pharmaceutical strategies [PEGylated (immuno)liposomal docetaxel, docetaxel–fibrinogen-coated olive oil droplets, docetaxel encapsulated nanoparticle–aptamer bioconjugates, submicronic dispersion formulation] to develop an alternative, solvent-free, delivery form for docetaxel characterized by increased efficacy and decreased toxicity.
aDepartment of Medical Oncology, Erasmus MC, Daniel den Hoed Cancer Center
bDepartment of Hospital Pharmacy and Clinical Pharmacology, Erasmus MC, University Medical Center, Rotterdam, The Netherlands
Correspondence to F.K. Engels, Department of Medical Oncology, Erasmus MC, Daniel den Hoed Cancer Center, University Medical Center, Groene Hilledijk 301, 3075 EA Rotterdam, The Netherlands
Tel: +31 10 4391 937; fax: +31 10 4391 053;
Received 27 June 2006 Revised form accepted 24 September 2006