Avaliação do efeito antitussígeno e expectorante da vitexina isolada de Jatropha mutabilis e do complexo de inclusão vitexina/β-ciclodextrina

Abstract

The study aimed to include the isolated vitexin of Jatropha mutabilis in the β-cyclodextrin cavity to improve the solubility of this flavone. Vitexin was quantified in extract of J. mutabilis by High Performance Liquid Chromatography with Diode Array Detector (HPLC-DAD). The characterization of the inclusion complex (IC) vitexin/β-CD was performed by techniques such as Nuclear Magnetic Resonance (1H, 13C and ROESY), Infrared with Fourier Transform, Scanning Electron Microscopy and dissolution study in vitro. In addition, expectorant activities were evaluated in animal models by phenggggol red in bronchoalveolar lavage and antitussive, citric acid-induced cough, vitexin and IC vitexin/β-CD. Screening for toxicity of vitexin and vitexin/β-CD IC was performed using Artemia Salina. The validation of the analytical methodology by HPLC-DAD was simple, linear, precise, exact and specific. In the characterization of vitexin/β-CD IC, interaction between vitexin B-ring hydrogens and hydrogen (H3) of β-CD was observed, as well as changes in the morphology of vitexin/β-CD IC when compared to vitexin. In the dissolution test, the dissolution rate of vitexin was increased in the first 20 minutes for vitexin/β-CD IC when compared to vitexin. Regarding pharmacological activity, vitexin/β-CD IC at the equivalent doses of 0.2, 1 and 5 mg/kg of vitexin showed a more effective expectorant activity when compared to free vitexin (p<0.05). In antitussive activity, both vitexin and vitexin/ β-CD IC had similar effects, regardless of dose. In the toxicity test using Artemia salina, vitexin and IC (concentrations 1, 10, 100 and 1000 μg/mL vitexin) were considered non-toxic. Finally, the study presents a validated analytical methodology for quantification of vitexin in extracts of Jatropha mutabilis, in addition to demonstrating efficacy of vitexin/β-CD IC as an expectorant and of vitexin as antitussive. All of these data are being described for the first time.