| Revue: | Brazilian Journal of Pharmaceutical Sciences |
| Base de datos: | PERIÓDICA |
| Número de sistema: | 000451791 |
| ISSN: | 1984-8250 |
| Autores: | Hadziabdic, Jasmina1 Spirtovic Halilovic, Selma1 Osmanovic, Amar1 Zahirovic, Lejla2 Elezovic, Amar3 |
| Instituciones: | 1University of Sarajevo, Faculty of Pharmacy, Sarajevo. Bosnia y Herzegovina 2KJP Veterinary Station Ltd., Sarajevo Microbiological-Chemical Laboratory for Testing and Examination of Food, Sarajevo. Bosnia and Herzegovina 3Agency for Drugs and Medical Devices, Control Laboratory Sarajevo, Sarajevo. Bosnia and Herzegovina |
| Año: | 2022 |
| Volumen: | 58 |
| País: | Brasil |
| Idioma: | Inglés |
| Tipo de documento: | Artículo |
| Enfoque: | Experimental, aplicado |
| Resumen en inglés | The aim of the present study is to improve the solubility and antimicrobial activity of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin by formulating its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin in solution and in solid state. The phase solubility study was used to investigate the interactions between 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin and 2-hydroxypropyl-β-cyclodextrin and to estimate the molar ratio between them. The structural characterization of binary systems (prepared by physical mixing, kneading and solvent evaporation methods) was analysed using the FTIR-ATM spectroscopy. The antimicrobial activity of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin and inclusion complexes prepared by solvent evaporation method was tested by the diffusion and dilution methods on various strains of microorganisms. The results of phase solubility studies showed that 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin formed the inclusion complexes with 2-hydroxypropyl-β-cyclodextrin of AP type. The solubility of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin was increased 64.05-fold with 50% w/w of 2-hydroxypropyl-β-cyclodextrin at 37 oC. The inclusion complexes in solid state, prepared by the solvent evaporation method, showed higher solubility in purified water and in phosphate buffer solutions in comparison with 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin alone. The inclusion complexes prepared by solvent evaporation method showed higher activity on Bacillus subtilis and Staphylococcus aureus compared to uncomplexed 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin due to improved aqueous solubility, thus increasing the amount of available 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin that crosses the bacterial membrane |
| Disciplinas: | Química |
| Palabras clave: | Química farmacéutica, Hidroxicumarinas, Ciclodextrina, Complejos de inclusión, Solubilidad de fases, Actividad antimicrobiana |
| Keyword: | Medicinal chemistry, Hydroxycoumarins, Cyclodextrin, Inclusion complexes, Phase solubility, Antimicrobial activity |
| Texte intégral: | Texto completo (Ver HTML) Texto completo (Ver PDF) |
