The effect of aliskerin loaded nanoparticles in experimental hypertension

Number of project: APVV- 0742-10

Coordinator: Oľga Pecháňová, ÚNPF SAV

Principal investigator: Ravingerová Táňa

Date: 1.5.2011 – 31.10.2014


Renin, the protease enzym, activates the renin- angiotensin – aldosterone system (RAAS) by cleaving angiotensinogen to yield angiotensin I, which is further converted into angiotensin II. Therefore, blockade of renin production may represnt an effective inhibition of whole RAAS. Aliskiren is the first in a class of drugs called direct renin inhibitor with high specifity. The limiting factor in clinical praxis might be, however, the relatively low bioavailability of aliskiren. The aim of this project is to decrease degradation and to increase bioavailability  of the renin inhibitor – aliskiren and to maximalize the effct of aliskiren on kidney function and structure. Decrease of  blood pressure will be thus effectively achieved by inhibition of the first step in RAAS activation. To increase bioavailability of aliskiren nanoencapsulation of this drug (nanoalis)  and magnetic nanoencapsulation will be performed followed by application and biological analysis of encapsulated aliskiren forms. While encapsulation assures decrease of degradation and increase of bioavailability, magnetization amplifies direct delivery of aliskiren to the target tissue of renin production – the kidney. By this way renoprotective effect of aliskiren besides blood pressure reduction will be achieved. In case of successful results, qualitatively new way in the treatment of hypertension and new drug discovery may be supposed.