Antihypertensive effect of carvacrol is improved after incorporation in β-cyclodextrin as a drug delivery system.

Abstract

Carvacrol (CARV), has been shown to possess various pharmacological properties, especially in the treatment of cardiovascular diseases. We evaluated the antihypertensive effect of the CARV free and encapsulation of CARV in β-cyclodextrin (CARV/β-CD), and whether CARV/β-CD is able to improve the antihypertensive effects of CARV free in spontaneously hypertensive rats (SHR). The rats were randomly divided into four groups, each treated daily for 21days and the mean arterial pressure and heart rate was measured every 5days: group 1, Wistar-vehicle solution; group 2, SHR-vehicle; group 3, SHR-CARV 50mg/kg/d; and group 4, CARV/β-CD 50mg/kg/d. After 21days of treatment, the mesenteric artery from treated animals was tested for phenylephrine (Phe) and sodium nitroprusside (SNP) sensitivity. In addition, administration of CARV/β-CD induced important antihypertensive activity when compared with the uncomplexed form, reducing the progression of arterial hypertension in SHR. Moreover, pharmacological potency to Phe in the SHR-CARV and CARV/β-CD groups was increased, approaching values expressed in the Wistar-vehicle. Furthermore, CARV/β-CD reduced the production of the pro-inflammatory mediator, IL-1β, and increased anti-inflammatory cytokine, IL-10. Together, these results produced evidence that the encapsulation of CARV in β-CD can improve cardiovascular activity, showing potential anti-inflammatory and antihypertensive effects.