Formulation and In-Vitro Evaluation of Dabigatran Etexilate Loaded Nanostructured Lipid Carriers

Abstract

The nanostructured lipid carriers (NLCs) is an interesting delivery system that can protect the encapsulated drugs and improve their dissolution, permeability and over all bioavailability. The aim of the present study was to prepare dabigatran etexilate (DAE)-encapsulated NLCs (DAE-NLCs) using glyceryl monostearate (GMS) and oleic acid (OA) as solid and liquid lipid matrix respectively, together with different surfactant types and ratios; DAE-NLCs were prepared using the hot emulsification-ultrasonication technique and the prepared formulations were characterized in terms of their particle size distribution, encapsulation efficiency (EE%), zeta potential, surface morphology and physical state characteristics. The prepared lipid nanoparticles shows a spherical shape with a particle size (62.4±5.75nm), poly dispersity index (PDI) of (0.286±0.001), zeta potential (-33.81±0.001 mV) the EE% was (92.42±2.31) and the drug loading capacity (LC %) was found to be (7.69±0.17). the in-vitro drug release study shows a bi-phasic drug release pattern with initial burst followed by a prolonged drug releasing phase with a 92% of the loaded drug was released in 24hr the release kinetics was fitted to Korsmyere-Peppas model with anomalous release mechanism. The solid state characterization depict an amorphous state of entrapped drug within the lipid matrix of the optimized DAE-NLCs. Short term stability study shows no significant change in nanoparticle characterization at refrigerator compared to room temperature. DAE-NLCs could be a potential delivery device for improved drug loading with controlled release properties that will improves oral bioavailability of the drug.

Keywords: Dabigatran Etexilate, Hot emulsification/ultrasonication, Nanostructured lipid carriers, Cremophor-EL.