Disposition kinetics, plasma protein binding, metabolism in vitro and in vivo of curcubitacins in rats

Abstract

Cayaponia tayuya (Vell.) Cogn of Cucurbitaceae family, native of throughout Brazil, has vast pharmacologycal potential scientifically proven as anti-tumor, anti-inflammatory and anti cancer due to the presence of cucurbitacines in roots of this plant.The species C. Tayuya have not established safety and efficacy and prolonged use or the use of high doses must be avoided until pharmacokinetic and toxicological studies are carried out. Pharmacokinetic preclinical evaluation aims to describe the parameters of absorption, distribution, metabolism and excretion of drugs in order to guide the design of clinical studies. The investigation of the biotransformation products in studies performed in vitro and in vivo aimed to predict the behavior of the drug candidate in humans, seeking to ensure greater security to the volunteers of studies clinical Phase I.Thus, the cucurbitacines drugs candidate should be evaluated as to the pre-clinical pharmacokinetic aspects, pharmacodynamic and toxicological tests, which form the basis of the expected effects in humans. The objectives of this project are to contribute in the development of drug candidates cucurbitacines through the characterization of preclinical pharmacokinetics, including research in models of metabolism in vitro and in vivo.