Exploring the potential of lecithin/chitosan nanoparticles in enhancement of antihypertensive efficacy of hydrochlorothiazide

Abstract

The present study involves the preparation of lecithin/chitosan nanoparticles loaded with hydrochlorothiazide (HCT) (a poorly water soluble antihypertensive) and hydrochlorothiazide complexed with β-cyclodextrin (HCT-β-CD) with a view to improve its biopharmaceutical properties. Nanoparticles prepared using modified solvent evaporation method showed a particle size in the range of 126–139 and 152–181 nm (polydispersity index, PDI = 0.2) for HCT and HCT-β-CD loaded nanoparticles respectively. TEM images revealed their spherical nature. The stable nature of the prepared formulations was evident from the high positive value of zeta potential (>20 mV). HCT and HCT-β-CD loaded nanoparticles with 150 mg of drug have shown a maximum entrapment efficiency of 81.8 ± 1.7% and 91.1 ± 1.5% respectively. In vitro studies have shown an improved and a sustained release pattern. In vivo activity in DOCA induced hypertensive rats demonstrates 1.5-fold percentage decrease in systolic blood pressure and a prolonged duration of action.

• poorly water soluble
• solvent evaporation
• nanotechnology
• zeta potential
• pharmacodynamics