Exploring the potential of lecithin/chitosan nanoparticles in enhancement of antihypertensive efficacy of hydrochlorothiazide.
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.
University Institute of Pharmaceutical Sciences, UGC Center of Advanced Study, Panjab University, Chandigarh, Punjab, India. renukchadha@rediffmail.com
Renu
R
Chadha
Swati
S
Bhandari
Darpan
D
Kataria
Sushma
S
Gupta
Dharamvir
D
Singh Jain
D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry*; D006852:Hydrochlorothiazide / Q000494:pharmacology*; D054709:Lecithins / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared
D000959:Antihypertensive Agents; D054709:Lecithins; D006852:Hydrochlorothiazide; D048271:Chitosan