Formulation and optimization of gefitinib-loaded nanosuspension prepared using a newly developed dendritic lipopeptide oligomer material

Abstract

Amino acid derived polypeptides are often biocompatible, and hence the materials of choice in nanoparticle formulations to avoid nanotoxicity and associated complications. A hydrophilic linear polypeptide γ-poly(l-glutamic acid) can form self-assembled nanoparticles only when made amphiphilic by chemical modification. Present work investigated pharmaceutical feasibility of a newly synthesized l-glutamic acid-based dendritic lipopeptide oligomer, which was found to be biocompatible and devoid of any inherent anticancer activity in vitro. Gefitinib, a poorly water-soluble anticancer drug, was used as the model drug to prepare an oligomeric nanosuspension by solvent evaporation–ultrasonication method. The formulation was optimized using response surface methodology and Box–Behnken model of design of experiments. The optimized gefitinib-loaded oligomeric nanosuspension demonstrated acceptable particle-size distribution, surface morphology, colloidal stability, entrapment efficiency, and drug release profile. Overall, current work highlights competence of a newly synthesized dendritic lipopeptide oligomer for drug delivery applications.