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

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 gamma-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.

Automated summary

This study investigates the pharmaceutical feasibility of a newly synthesized amino acid-derived polypeptide for drug delivery, demonstrating its potential in preparing nanosuspensions and successfully loading the anticancer drug, gefitinib.