In-vitro – In-vivo Characterization of ‎Glimepiride Lipid Nanoparticulates ‎Prepared by Combined Approach of ‎Precipitation and Complexation

Novel lipid nanoparticulates (NCs) were developed by a combined approach of precipitation and complexation with an aim to improve the solubility, stability and targeting efficiency of glimepiride (GLP). GLP NCs were prepared by precipitation process using PEG 20000 and further complexed with phospholipon90G (P90G). The NCs were evaluated for physicochemical characterization, such as drug loading, saturation solubility (SS) and particle characterization studies. The solid state characterization studies were performed using X-ray powder diffractometry (XRPD), differential scanning calorimetry (DSC), infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). Further in-vitro dissolution studies and in vivo (drug targeting) studies were also performed. Short term (3 months) stability studies were conducted on most satisfactory NCs. GLP P90G NCs exhibited three folds increase in saturation solubility. Particle size of NCs was ranging from between 210-240 nm. The dissolution and in vitro stability of NCs were superior compared to pure GLP. XRPD and DSC analysis proved that crystallinity prevailed in NCs, but with a slight change in crystal structure. SEM analysis indicated spherical shaped particles with a lipid coat. The NCs were found to be stable during the period of study. In vivo studies on optimized NCs showed slightly higher drug concentration (1.38 µg/ml) in pancreas of rat than that of pure GLP. It can be concluded that solubility and stability of GLPNCs were significantly improved by P90G complexation. Also, P90G (phospholipids) could be effectively used in enhancing the targeting efficiency and pharmacokinetics of glimepiride.