Development and Characterization of Glimepiride-Loaded Polymeric Nanoparticles: Formulation Design and Evaluation

Abstract

Purpose

This study was aimed to develop polymeric nanoparticles (PNPs) using chitosan (CTN), polyvinyl pyrrolidone (PVP), and Tween 80 for dissolution enhancement of poorly water-soluble antidiabetic drug: glimeperide (GLM).

Methods

GLM-loaded PNPs were developed for increasing the dissolution and solubility of GLM by using different amounts of CTN as polymer, PVP, and Tween 80 as stabilizers and tri-polyphosphate (TPP) as a crosslinking agent. PNPs were prepared using a combined approach of solvent evaporation and ionic gelation techniques. The newly fabricated PNPs were further characterized for percent encapsulation efficiency (%EE), compatibility studies, average particle size, morphology, thermal behavior, XRD examination, and dissolution studies at different biorelevant pH conditions.

Results

The prepared PNPs showed % encapsulation efficiency in the range of 55.90 to 93.25%. Fourier transform infrared studies revealed compatibility of GLM with formulation composites. The optimized PNPs F_1PVP and F_4TW80 showed particle size in nanoscale range 323 nm and 149 nm, respectively. SEM indicated formation of irregular (flakes) shaped particles. DSC and PXRD studies revealed reduction in crystallinity of the GLM inside PNPs thus promoting the dissolution. The dissolution studies at biorelevant acidic pH 1.2 and biorelevant basic pH 6.8 demonstrated remarkable improvement in dissolution profile compared to pure aqueous dispersion of GLM.

Conclusion

Overall results of the study suggested that CTN-based PNPs stabilized with PVP and Tween 80 can act as promising carriers for oral drug delivery of GLM.