Formulation of Stable Nanoliposomes of Docetaxel: Design, Optimization, and in-vitro Characterization

Abstract

Background: Liposome offers many advantages over conventional dosage forms, like increased bioavailability, possibility of releasing drug at slower and constant rate, accurate drug release. Docetaxel is approved by the FDA for the treatment of locally advanced or metastatic breast cancer, head and neck cancer, gastric cancer. Docetaxel is BCS Class 4 drug; hence efficacy can be improved with liposomal formulation. Objectives: The Present study prepared Docetaxel loaded liposomal formulation. Materials and Methods: Formulation batches were designed on the basis of solvent, lipid to cholesterol ratio, lipid to release modifier ratio, hydration temperature and various physicochemical and morphological properties of formulation were examined. The zeta potential, particle size determination, pH, stability, determination of encapsulation efficacy, morphology of formulation and in-vitro drug release were investigated. Results:  The zeta potential values of FD5 and FD9 were found to be -12.6 to -12.9 mV and -10.6 to -11.9 mV respectively. The entrapment efficiency of formulations of batch FD5 and FD9 were found to be 83.20% and 85.22% respectively. By comparing both FD5 and FD9 it was found that FD9 batch is optimized than FD5 in all aspects.  The formulation batch FD9 has particle size of 105 nm, zeta potential in range of -10.6 to -11.9 mV; Drug entrapment efficiency 85.22%, Assay of formulation was 99.56 % and FD9 formulation shows extended release of Drug up to 13 hours. Conclusion: The study confirmed that the Liposome formulation was successfully prepared and evaluated.