Formulation Development, Optimization and Evaluation of Imipramine Loaded Nano-Structured Lipid Carrier

Abstract

Background: Nano-structure Lipid Carriers (NLCs) are small spheres extending in scale from 10 to 1000 nanometres comprised of biocompatible and biodegradable lipids. These spheres can encapsulate both hydrophilic and lipophilic drugs, preserving them from degradation and increasing their distribution to the intended place in the body. Imipramine, a tricyclic antidepressant, has been investigated in hamster model at 5-10 mg/kg for experimental leishmaniasis. The goal of this research is to develop Imipramine in a nano-structured lipid carrier formulation for targeting macrophage cells.Materials and Methods: Imipramine-loaded NLCs were created employing Glyceryl Monostearate (GMS) as the solid lipid constituent alongside oleic acid as the liquid lipid, while tween80 acted as the surfactant. The process of hot homogenization was employed to prepare the NLCs. The formulation was optimized using 23 factorial designs using design expert software. The optimised formulation was further used for the preparation of mannose functionalized imipramine-loaded NLCs.Results: The IMP-NLC opt and M-NLC show a globule size of 348.5±0.81 nm and 459.4±0.28 nm with encapsulation efficiency of 61.6±0.326% and 64.48±0.408%, respectively. The drug release in vitrodemonstrates a dual-phase pattern, featuring an early rapid sudden release followed by a gradual and slower release. The surface morphology, drug release kinetics and stability were also used to characterize the prepared NLCs.Conclusion: This study concludes that nanostructured lipid carriers demonstrate considerable encapsulation efficiency, release and stability for further pre-clinical investigation.

Keywords: Imipramine; Nanostructure lipid carrier; 23 factorial design; Particle size; Encapsulation efficiency