Optimized Vildagliptin Microsphere Formulation and in vitro Characterization Using 23 Factorial Design Analysis

Background:

Vildagliptin is a dipeptidyl peptidase-4 inhibitor employed for the intervention of non-insulin-dependent diabetes mellitus which has a short half-life. The intention of this work is to devise and qualify vildagliptin microspheres to analyse the impact of two different-polymers, encapsulating agents, and stirring speeds for sustained drug release.

Materials and Methods:

The formulations were crafted by method of solvent evaporation and developed by applying 2³ complete factorial designs. The independent variables are the polymers (X1), encapsulating agents (X2) and stirring speed (X3). The dependent variables are particle size (Y1), degree of swelling (Y2), encapsulation efficiency (Y3), in vitro drug release studies (Y4). The kinship between independent and dependent variables were demonstrated using response surface diagrams. Additionally, the formulated microspheres were analysed for the parameters practical yield, kinetics of drug release and morphology.

Results:

The particle size and degree of swelling of microspheres were influenced substantially by the hydrophilic characteristic of the polymer used. The loading efficiency and the percentage of drug release was found to be ameliorated in water insoluble Eudragit RS 100 microspheres. The microspheres batch VGM6 prepared was observed to be suitable in accordance with loading efficiency 76.3% and slow percentage of drug release 71.78% in 8 hr following Hixson-Crowell kinetics and was characterized by SEM for morphology.

Conclusion:

The similarity and dis-similarity factors show that the rate of drug profiles were similar to each other and the formulation releases the drug slower than that of the innovator brand.