MORPHOLOGY OF POLYSORBATE 80 MICELLES DERIVED FROM INJECTABLE DOCETAXEL 40 MG/ML

Abstract

Docetaxel is a semi-synthetic drug from the taxane family that has demonstrated effective antitumor activity and its use has been approved for the local treatment of patients with various types of human cancer. It is administered by slow intravenous infusion in saline, so it is essential to study its stability in solution. The effectiveness of the active pharmaceutical ingredient docetaxel is limited by its low solubility in water. One of the solutions to facilitate its use is through polysorbate 80 micellar systems as a vehicle for parenteral administration. Laboratorios aica+ (Cuba) produces and markets docetaxel in the form of a micellar system composed of a concentrate for intravenous infusion together with its corresponding diluent (Docetaxel 40 mg/mL). In the current work the morphology of polysorbate 80 micelles derived from the injectable Docetaxel 40 mg/mL was studied. Micellar systems of the injectable in water, 5% dextrose saline and 0.9% sodium chloride saline were prepared and the critical micelle concentration was calculated from a spectrophotometric and a conductometric method. In addition, the hydrodynamic diameter and the Z potential were determined in samples prepared in physiological sera from measurements made by dynamic light scattering. It was obtained that the values of critical micellar concentration and hydrodynamic diameters are adequate for the parenteral administration of the drug under study, while the Z potential values indicate that the product may be unstable in solution.