A Systematic Approach to Vildagliptin-Eudragit RL 100 Coated Nanoparticles by Combined Techniques of Solvent Evaporation and Nano-precipitation Using Quality by Design Concept

Abstract

Background: Diabetes is an endocrine disorder characterized by an abnormal increase in blood sugar level. Vildagliptin is a Dipeptidyl Peptidase-4 (DPP-4) inhibitor used in the treatment of type 2 diabetes mellitus.Purpose: The present work deals with the Quality by Design (QbD) approach based formulation and optimization of Vildagliptin-Eudragit RL 100 coated nanoparticles (VLD-EudNPs).Materials and Methods: VLD-Eud NPs were developed by combined technique of solvent evaporation and nano-precipitation. Optimization was done by 32 factorial designs. Prepared nanoformulations were characterized for percentage yield and morphology. Further in vitro drug release and kinetics were studied. The accelerated stability study of the optimized formulation was carried out for 3 months.Results: VLD-EudNPs ranged from 58.5±2.02 nm to 425.4±4.71 nm with a PDI of 0.27±0.036 to 0.52±0.086. Entrapment efficiency (% EE) of nanoformulations F1 to F9 ranged between 32.29±1.16 to 75.26±1.63%. The particles were found to be cylindrical-shaped, with a percentage yield of 54.7±3.45 to 84.4±1.51%. During the in vitro drug release study, at acidic pH, <5% drug release, while delayed release at basic pH, at the end of 24 hr, all formulations have released >68% of the drug following zero order kinetics. The optimized formulation has proven its stability during stability study.Conclusion: The present work concludes that prepared and optimized VLD-Eud NPs could be a better approach for sustained delivery of Vildagliptin for the management of diabetes mellitus as compared to traditional drug delivery.

Keywords: Polymeric nanoparticles; Vildagliptin; Quality by Design; Diabetes