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Abdus Samad

Title: Systematic development of nanolipospheres loaded with phospholipid complex of rosuvastatin with enhanced biopharmaceutical performance

Abdus Samad

Panjab University, India

Biography

Updated Soon..

Abstract

The present work describes the development and characterization of novel nanolipospheres-loaded with phospholipid-drug complex of rosuvastatin calcium with distinctly improved oral biopharmaceutical performance. The equilibrium solubility study of the rosuvastatin was carried out in various phospholipids and explored for preparing molecular complexes with the help of Job’s plot. Physiochemical characterization of the complex was carried out employing FTIR, H1-NMR, DSC and PXRD techniques, which confirmed the formation of phospholipid complex. Application of molecular modeling and simulation techniques facilitated precise identification of possible binding site(s) in phospholipid for complexation of drug molecules on it. Evaluation of complex through solubility studies and in vitro drug release revealed 2.14-fold augmentation in the solubility vis-à-vis the pure drug. Further, the lipid-drug complex was loaded into the nanolipospheres using phase inversion method. The nanolipospheres were optimized through response surface methodology using Box-Behnken design, evaluating them for particle size, zeta potential, entrapment efficiency and drug release. Mathematical modeling of the experimental data was carried out by fitting with second-order quadratic model followed by optimum search through numerical optimization and desirability function. The prepared formulations were also evaluated for ex vivo permeation and in situ intestinal perfusion studies indicating nearly 3.35-fold improvement in the permeability and absorption parameters of the drug from complex loaded in nanolipospheres vis-à-vis the plain complex and pure drug. In vivo pharmacokinetic and lymphatic distribution studies also construed significant improvement in the distribution of drug through lymph followed by absorption into the systemic circulation from the complex loaded in nanolipospheres vis-à-vis the plain complex and pure drug. In a nutshell, the above studies succesffully demonstrated the enhanced biopharmaceutical performance of rosuvastatin calcium from the novel complex-loaded in nanolipospheres.