| خلاصه مقاله | Introduction: 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 drug for reducing BP. In
this study, single-pass intestinal perfusion (SPIP) technique was used for investigating the
intestinal permeability of Valsartan. The aim of this study was to increase intestinal
permeability of valsartan loaded in Nano-emulsions and solid Lipid Nanoparticles.
Method & material:SPIP was performed in isolated jejunal segments at three Formulation
of Valsartan (PEGylated SLN, Non- PEGylated SLN, and Nanoemulsion) 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 Valsartan could be attributed to intestinal absorption. Outlet samples were analyzed
using the developed HPLC method and effective permeability values were calculated by
respected formula.
Result: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 Nano emulsion 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.
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 bioavailability. New
techniques have shown that the use of nanoparticles like SLNs and nanoemulsions can
dramatically increase intestinal permeability. |