Fabrication of Lipid Combination for Bioavailability Enhancement of Isoniazid

Abstract

The objective of this work was to precisely design novel lipid composition and investigate for improved characteristics to enhance the bioavailability of isoniazid (INH) loaded in nanostructured lipid carrier (NLC). Response surface methodology (RSM)-Central composite rotatable design (CCRD) was used to evaluate the effect of formulation variables, the ratio of two different solid lipids, solid lipid: liquid lipid, and the drug concentration on response variables. The encapsulation efficiency (EE) of optimized formulation was found to be 72.82±0.49%, drug loading (DL) was 15.15±0.10%, mean particle size (PS) was 285.1±4.71nm and in vitro drug release (DR) was 75.30±1.95% in 24 h. The optimized formulation was investigated via Differential Scanning Calorimetry (DSC), X-Ray Diffraction Pattern (XRD) analysis, in vitro release kinetics and Transmission electron microscopy (TEM). The polydispersity index (PDI) and zeta potential (ZP) were determined as 0.484±0.026 and +21±1.44mV respectively. Formulations were found to be most stable up to 25°C for 6 months. The present study successfully optimized the lipid combination at different concentrations and introduced the best composition of lipids with improved characteristics of INH-NLC formulation and expected to increase the bioavailability of isoniazid to replace the conventional drug delivery system for tuberculosis.