In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
by
Eleonore Haltner-Ukomadu 1,*, Svitlana Gureyeva 2, Oleksii Burmaka 2,*, Andriy Goy 2, Lutz Mueller 3,*, Grygorii Kostyuk 2 and Victor Margitich 2
Eleonore Haltner-Ukomadu 1,*, Svitlana Gureyeva 2, Oleksii Burmaka 2,*, Andriy Goy 2, Lutz Mueller 3,*, Grygorii Kostyuk 2 and Victor Margitich 2
1
Across Barriers, Science Park 1, 66123 Saarbruecken, Germany
2
Joint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, Ukraine
3
Dr. Regenold GmbH, Zoellinplatz 4, 79410 Badenweiler, Germany
*
Authors to whom correspondence should be addressed.
Sci. Pharm. 2018, 86(1), 3; https://doi.org/10.3390/scipharm86010003
Received: 11 October 2017 / Revised: 5 January 2018 / Accepted: 8 January 2018 / Published: 11 January 2018
An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability (Papp) of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1.2 to 7.5 is about 60 mg/mL at 25 °C, and ranges from 130 to 150 mg/mL at 37 °C, depending on the pH. Based on these results, enisamium iodide can be classified as highly soluble. Enisamium iodide demonstrated low permeability in Caco-2 experiments in all tested concentrations of 10–100 μM with permeability coefficients between 0.2 × 10−6 cm s−1 and 0.3 × 10−6 cm s−1. These results indicate that enisamium iodide belongs to class III of the Biopharmaceutics Classification System (BCS) due to its high solubility and low permeability. The bioavailability of enisamium iodide needs to be confirmed in animal and human studies.
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MDPI and ACS Style
Haltner-Ukomadu, E.; Gureyeva, S.; Burmaka, O.; Goy, A.; Mueller, L.; Kostyuk, G.; Margitich, V. In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide. Sci. Pharm. 2018, 86, 3.
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