Absorption enhancement effect of piperine and chitosan on ganciclovir sol-id lipid nanoparticles: formulation, optimization and invivo pharmacoki-netics

Abstract

The purpose of the present study was to formulate Solid Lipid Nanoparticles (SLNs) of Ganciclovir (GCV) in combination with Chitosan and Piperine for absorption enhancement effect. GCV loaded SLNs were prepared by hot homogenization method, optimized and characterized. Formulated SLNs were incorporated with absorption enhancers and characterized for invitro absorption (with chicken intestine), histopathological and invivo pharmacokinetic studies. Invitro absorption studies revealed that the permeability coefficient of the prepared formulation is more when compared to the pure drug, so the permeability is more for prepared formulation. In vivo pharmacokinetic study showed a significant increase in the Cmax, AUC, biological half-life and decrease in elimination rate constant for prepared formulation compared to pure drug. Histopathological studies also showed mild reversible damage of epithelial cells with Chitosan which indicates the safety and efficacy of the formulation. Thus, GCV loaded SLNs prepared with Chitosan can be clinically promising for enhancing the oral, intestinal absorption of the said BCS Class-III drug.

Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

“…Regarding antiviral formulations intended for systemic effect after oral administration (Gaur et al, 2014;Shi et al, 2015;Ravindra Babu et al, 2019), an interesting work by Ravi et al (2014) evaluated the comparative performance of the protease inhibitor lopinavir (LPV)-SLN with respect to LPV alone and the combination of LPV-Ritonavir (RTV). LPV is co-formulated with subtherapeutic doses of Ritonavir to overcome its poor oral BA due to CYP3A4 metabolism and P-glycoprotein (P-gp) efflux, both inhibited by RTV.…”