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Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12128/7084
Title: Enhanced pharmacological efficacy of sumatriptan due to modification of its physicochemical properties by inclusion in selected cyclodextrins
Authors: Paczkowska, Magdalena
Mizera, Mikołaj
Sałat, Kinga
Furgała, Anna
Popik, Piotr
Knapik-Kowalczuk, Justyna
Paluch, Marian
Krause, Anna
Szymanowska-Powałowska, Daria
Fojud, Zbigniew
Kozak, Maciej
Cielecka-Piontek, Judyta
Keywords: sumatriptan; pharmacological action
Issue Date: 2018
Citation: Scientific Reports, Vol. 8, iss. 1 (2018), Art. No. 16184
Abstract: The study focused on the pharmacological action of sumatriptan, in particular its antiallodynic and antihyperalgesic properties, as an effect of cyclodextrinic inclusion of sumatriptan, resulting in changes of its physicochemical qualities such as dissolution and permeability through artificial biological membranes, which had previously been examined in vitro in a gastro-intestinal model. The inclusion of sumatriptan into β-cyclodextrin and 2-hydroxylpropylo-β-cyclodextrin by kneading was confirmed with the use of spectral (fourier-transform infrared spectroscopy (FT-IR); solid state nuclear magnetic resonance spectroscopy with magic angle spinning condition, 1H and 13C MAS NMR) and thermal (differential scanning calorimetry (DSC)) methods. A precise indication of the domains of sumatriptan responsible for its interaction with cyclodextrin cavities was possible due to a theoretical approach to the analysis of experimental spectra. A high-performance liquid chromatography with a diode-array detector method (HPLC-DAD) was employed to determine changes in the concentration of sumatriptan during dissolution and permeability experiments. The inclusion of sumatriptan in complex with cyclodextrins was found to significantly modify its dissolution profiles by increasing the concentration of sumatriptan in complexed form in an acceptor solution compared to in its free form. Following complexation, sumatriptan manifested an enhanced ability to permeate through artificial biological membranes in a gastro-intestinal model for both cyclodextrins at all pH values. As a consequence of the greater permeability of sumatriptan and its increased dissolution from the complexes, an improved pharmacological response was observed when cyclodextrin complexes were applied.
URI: http://hdl.handle.net/20.500.12128/7084
DOI: 10.1038/s41598-018-34554-w
ISSN: 2045-2322
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