Desenvolvimento de sistema de nanoemulsão contendo geraniol com a avaliação da sua atividade in vivo e in vitro para o tratamento de desordens gastrointestinais e respiratórias

Abstract

Geraniol (GE) is a major monoterpene in some plant species used in folk medicine and has relevant pharmacological properties, including antitumor, anti-inflammatory, antioxidative, antimicrobial, hepatoprotective, cardioprotective and neuroprotective effects. Despite the extensive description of its effects, the activity of EG in the treatment of respiratory and gastrointestinal disorders has not been explored, nor in nanoemulsion systems, which in turn improve the ability to deliver drugs in biological systems. In this way, EG and its nanoformulation were evaluated in in vitro and in vivo models for their pharmacological activity in these two physiological systems. For the in vitro evaluation, cumulative concentrations of EG and its nanoemulsion (1.0 x 10-7-3.0 x 10-3 M) were tested in samples of ileum and trachea isolated from guinea pigs. In the in vivo model, doses of 10, 50, 100, 200 and 400 mg/kg were used in a model of diarrhea induced by ricin oil, gastrointestinal transit speed with added charcoal and cough induced by acetic acid at doses of 100, 200 and 400 mg/kg and with evaluation of sub-acute toxicity at a dose of 2000 mg/kg. The results showed that GE had spasmolytic activity in the ileum in carbacol-induced contractions, with a possible mechanism of action involving the BKCa and TRPV1 channels, with its pharmacological potency increased with the formulation (F1) of the monoterpene in its nanoemulsion system. EG showed an anti-diarrheal effect in mice at doses of 200 and 400 mg/kg, with an increase in its pharmacological potency in its nanoemulsion at all doses, which in turn showed a reduction in intestinal transit speed at doses of 200 and 400 mg/kg. GE showed no toxicity or spasmolytic activity in isolated guinea pig trachea, but did show antitussive activity at doses of 100 and 200 mg/kg compared to codeine. [Thus, GE is a monoterpene with biotechnological potential, as is its nanoemulsion system, for gastrointestinal disorders.