DEVELOPMENT AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES OF LINAGLIPTIN

The main objective of the present research work was to formulate and characterize the linagliptin-loaded solid lipid nanoparticles (SLNs). SLNs possess distinctive characteristics like small and spherical shapes with an average diameter between 1to 100 nm. Linagliptin is used for the treatment of type II diabetes and it is a dipeptidyl peptidase 4-inhibitor and its oral bioavailability is 30%. The application of biopharmaceutical principles to the physicochemical properties of drug substance are characterized with the goal of designing best drug delivery system. The current research work was to enhance the oral bioavailability of linagliptin using the different phospholipids like stearic acid, glyceryl monostearate, cholesterol along with the surfactants like tween 80, span 80, poloxamer1 88, and span 20 by solvent emulsification/solvent evaporation method and solvent emulsification method in order to obtain the best novelty formulation. The prepared formulations have been evaluated for particle size analysis, zeta potential, percentage drug entrapment efficiency, scanning electron microscopy studies, in-vitro drug release kinetics, and stability studies. FT-IR spectra showed the there was no incompatibility between linagliptin and excipients. Formulations containing glyceryl monostearate and surfactants like poloxamer188 showed smaller particle size, greater drug release, and higher percentage entrapment efficiency. The best formulation F10, exhibited 687.2 nm particle size and 99.25% drug release.