Eremantholide C from aerial parts of Lychnophora trichocarpha, as drug candidate : fraction absorbed prediction in humans and BCS permeability class determination.
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2021
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Background Lychnophora trichocarpha (Spreng.) Spreng. ex Sch.Bip has been used in folk medicine to treat pain, inflammation,
rheumatism and bruises. Eremantholide C, a sesquiterpene lactone, is one of the substances responsible for the anti-inflammatory
and anti-hyperuricemic effects of L. trichocarpha.
Objectives Considering the potential to become a drug for the treatment of inflammation and gouty arthritis, this study evaluated
the permeability of eremantholide C using in situ intestinal perfusion in rats. From the permeability data, it was possible to predict
the fraction absorbed of eremantholide C in humans and elucidate its oral absorption process.
Methods In situ intestinal perfusion studies were performed in the complete small intestine of rats using different concentrations
of eremantholide C: 960 μg/ml, 96 μg/ml and 9.6 μg/ml (with and without sodium azide), in order to verify the lack of
dependence on the measured permeability as a function of the substance concentration in the perfusion solutions.
Results Eremantholide C showed Peff values, in rats, greater than 5 × 10−5 cm/s and fraction absorbed predicted for humans
greater than 85%. These results indicated the high permeability for eremantholide C. Moreover, its permeation process occurs
only by passive route, because there were no statistically significant differences between the Peff values for eremantholide C.
Conclusion The high permeability, in addition to the low solubility, indicated that eremantholide C is a biologically active
substance BCS class II. The pharmacological activities, low toxicity and biopharmaceutics parameters demonstrate that
eremantholide C has the necessary requirements for the development of a drug product, to be administered orally, with action
on inflammation, hyperuricemia and gout.
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Insituperfusion, Biopharmaceutics, Classification system
Citação
CALDEIRA, T. G. et al. Eremantholide C from aerial parts of Lychnophora trichocarpha, as drug candidate: fraction absorbed prediction in humans and BCS permeability class determination. DARU Journal of Pharmaceutical Sciences, v. 29, p. 195-203, 2021. Disponível em: <https://link.springer.com/article/10.1007/s40199-021-00397-6>. Acesso em: 11 out. 2022.