Preparation and Intestinal permeability studies on Valsartan Nano-emulsions and Solid Lipid Nanoparticles

Abstract

Introduction and Background: Cardiovascular diseases are one of the leading causes of death in different parts of the world. Hypertension, sometimes called arterial hypertension, is a chronic condition in which the blood pressure in the arteries rises. Angiotensin II receptor blockers are mainly used for treatment of CVD. Valsartan is a class III ARB drugs for reduce of BP. In this study single-pass intestinal perfusion (SPIP) technique was used for investigating the intestinal permeability of Valsartan. Aim: The aim of this study was to increase intestinal permeability of Valsartan loaded in Nano-emulsions and Solid Lipid Nanoparticles Methods: SPIP was performed in isolated jejunal segment at three Formulation of Valsartan (PEGylated SLN, Non-PEGylated SLN and Nano emolsion) to compare intestinal permeability changes against of simple solution of Valsartan. Phenol red was used as a non-absorbable marker. Stability studies were conducted to ensure that the loss of Valsatan could be attributed to intestinal absorption. Outlet samples were analysed using the developed HPLC method and effective permeability values were calculated by respected formula. Results: The effective permeability value of Valsartan simple solution in the jejunum was 4.129×10-3. Also the effective permeability values of PEGylated and non-PEGylated SLNs and Valsartan nanoemolsoin were found to be 1.7119×10-2, 1.442×10-2 and 1.299×10-2 cm/sec. The use of nanoparticle formulations led to a significant increase in intestinal permeability of Valsartan. Discussion and conclusion: In conclusion, Valsartan can be absorbed only 23% in the intestine. The high aqueous solubility of Valsartan might be a crucial factor for its poor oral bioavailability. New techniques have shown that the use of nanoparticles like SLNs and nanoemolsion can dramatically increase intestinal permeability.