Formulation, Characterization, and Pharmacokinetic Evaluation of Novel Glipizide-phospholipid Nano-complexes with Improved Solubility and Bio-availability

Abstract

Background: The proposed study was aimed to formulate and evaluate the Glipizide-Phospholipid Nano-complex. Since Glipizide is a poorly soluble drug, its complexation with phospholipids is an ideal approach to improving solubility Method: To improve the oral potency of Glipizide, its phospholipid complex was prepared by employing the solvent evaporation method. The formulations were characterized using DSC, FT-IR, PXRD, SEM, TEM, and hot stage microscopy (HSM). Solubility tests of the Glipizide-Phospholipid Nano-complex revealed a significant increase in aqueous solubility compared to Glipizide's physical combination. The oral bioavailability of the Glipizide-Phospholipid Nano-complex was measured by using HPLC in Wistar rats’ plasma. FTIR and PXRD results revealed no significant interaction between the drug and the phospholipid in the formulation. SEM and TEM studies confirmed the morphology of the formulation assuring the conversion of crystalline form into an amorphous structure. Results: The Glipizide-Phospholipid Nano-complex had a greater peak plasma concentration (5.2 vs 3.8 g/mL), a larger AUC (26.31 vs 19.55 μgh/L), and a longer T1/2 (2.1 vs 4.1 h) than free Glipizide, indicating that it improved drug dissolution rate. Conclusion: The outcomes suggested that a phospholipid complexation is a potential approach to increasing water-insoluble drugs' oral bioavailability.

Novel Phytosomal Formulation of Emblica officinalis Extracts with Its In Vivo Nootropic Potential in Rats: Optimization and Development by Box-Behnken Design

“…EOE's higher wettability and solubility in the prepared phytosome may account for the considerable diference in the EOP release rate between EOE and PM. Te following facts could explain this: (1) in the EOP, EOE transitions from a crystallized to a partially amorphous form, extending the pace and extent of breakdown to 12 hours, (2) improved solubility of EOE owing to the amphiphilic nature of LECIVA S 70, and (3) increased wettability and improved dispersion of EOP due to changes in the structural morphology of crystalline EOE into partial amorphization imparted due to the amphiphilic nature of LECIVA S 70 phospholipid [16,31].…”

“…Te enhancements in bioavailability in plasma after single oral dose administration of EOP are attributed to forming of molecular aggregates with amphiphilic phospholipid, improving aqueous solubility and enhancing intestinal absorption. Phospholipids are amphiphilic and can shield EOE from frst-pass metabolism in the liver and increase bioavailability [16,31].…”