Exploring Lecithin/Chitosan Nanoparticles of Ramipril for Improved Antihypertensive Efficacy

Author： Chadha Renu Bhandari Swati Kataria Darpan Gupta Sushma

Publisher： American Scientific Publishers

ISSN： 2167-9320

Source： Journal of Nanopharmaceutics and Drug Delivery, Vol.1, Iss.2, 2013-06, pp. : 173-181

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Abstract

Ramipril, a widely used therapeutic agent used in the treatment of hypertension, exhibits poor aqueous solubility resulting in low oral bioavailability. The present study is focused on optimizing this important physicochemical property by entrapping the drug into the nanoparticles. Besides this, drug complexed with beta-cyclodextrin is also incorporated in nanoparticles. The lecithin/chitosan nanoparticles prepared using solvent evaporation method were characterized for their particle size, shape, surface charge, entrapment efficiency and in-vitro drug release. In-vivo antihypertensive activity in deoxycorticosterone acetate salt induced hypertensive rats was performed to assess the therapeutic efficacy. A particle size of 183 ± 0.5 (ramipril nanoparticles) and 199 ± 1.5 nm (ramipril-β-CD nanonanoparticles) and a high entrapment efficiency of above 72.3% were achieved. The nanoparticles were spherical in shape and exhibited a high positive value of zeta potential (> 30 mV) which indicated the stability of the prepared formulations. A significantly improved in-vitro drug release in comparison to the free drug was observed which followed Peppas release pattern (r² = 0.997). In vivo activity in deoxycorticosterone acetate salt induced hypertensive rats demonstrated 1.6 fold percentage decrease in systolic blood pressure. The prepared lecithin/chitosan NPs represent an efficient new drug delivery system for oral administration of this poorly water soluble drug.