Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels

The aim of our study was to identify factors affecting the in vitro release of diclofenac sodium (DS) from hypromellose-based gels (HPMC). Materials and methods. Gels with HPMC and liquids without HPMC were studied by viscosity-rotating viscometer method and spin probe electron paramagnetic reson...

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Autores principales:	Elena Bezuglaya, Hanna Ivashchenko, Nikolay Lyapunov, Igor Zinchenko, Anna Liapunova, Yurij Stolper, Oleksii Liapunov, Tetiana Pukhova
Formato:	article
Lenguaje:	EN
Publicado:	PC Technology Center 2021
Materias:	hypromellose gel liquid diclofenac sodium isopropyl alcohol viscosity rotational correlation time (τ–1) in vitro release test (ivrt) Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/5eeae36c2b114ddd9a55884a31867287
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spelling	oai:doaj.org-article:5eeae36c2b114ddd9a55884a318672872021-11-04T14:22:47ZStudy of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels2519-48442519-485210.15587/2519-4852.2021.243040https://doaj.org/article/5eeae36c2b114ddd9a55884a318672872021-10-01T00:00:00Zhttp://journals.uran.ua/sr_pharm/article/view/243040https://doaj.org/toc/2519-4844https://doaj.org/toc/2519-4852The aim of our study was to identify factors affecting the in vitro release of diclofenac sodium (DS) from hypromellose-based gels (HPMC). Materials and methods. Gels with HPMC and liquids without HPMC were studied by viscosity-rotating viscometer method and spin probe electron paramagnetic resonance spectroscopy. Rheograms were used to determine the flow behavior and the apparent viscosity, and the EPR spectra were used to determine the rotational correlation time (τ–1) of the dissolved spin probes. The in vitro release tests were performed using vertical diffusion cells according to a validated procedure. The assay of DS and isopropyl alcohol (IPA) in the receptor medium was performed by high performance liquid chromatography (HPLC) and gas chromatography (GC) according to validated procedures, and the water content was determined using semi-micro method. Results. The apparent viscosity of the gels increased with increasing HPMC content and depended on the HPMC grade. The high apparent viscosity of the gels did not affect the values of τ–1 of the dissolved spin probes. In viscous gels and Newtonian fluids, the composition of which corresponded to the dispersion medium of gels, the values of τ–1 were identical and were in the range of rapid rotation, which is a prerequisite for similar and rapid release of the dissolved substances from gels and liquids. It was shown that the HPMC-based gel and Newtonian liquid without HPMC in terms of in vitro release parameters DS and IPA were equivalent. During in vitro testing the release of dissolved DS increased with increasing its concentration in the gel and depended on the dispersed state of DS. When the content of IPA was changed from 45.0 % to 22.5 %, the water absorption by the gel and the release of IPA decreased, and the release of DS increased, which was due to the decrease in the solubility of DS in the gel. Conclusions. HPMC, which provided high apparent viscosity of the gels, did not affect the value of τ–1 of the dissolved spin probes and the in vitro release of DS from the gels. The gel and Newtonian liquid were equivalent in terms of in vitro release of DS and IPA. The release of DS altered proportionally with the concentration of DS and depended on its dispersed state. As the content of IPA decreased, the release of IPA decreased, but the release of DS increased because of the decrease in the solubility of the DS in the gelElena BezuglayaHanna IvashchenkoNikolay LyapunovIgor ZinchenkoAnna LiapunovaYurij StolperOleksii LiapunovTetiana PukhovaPC Technology Centerarticlehypromellosegelliquiddiclofenac sodiumisopropyl alcoholviscosityrotational correlation time (τ–1)in vitro release test (ivrt)Pharmacy and materia medicaRS1-441ENScienceRise: Pharmaceutical Science, Iss 5(33), Pp 12-31 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	hypromellose gel liquid diclofenac sodium isopropyl alcohol viscosity rotational correlation time (τ–1) in vitro release test (ivrt) Pharmacy and materia medica RS1-441
spellingShingle	hypromellose gel liquid diclofenac sodium isopropyl alcohol viscosity rotational correlation time (τ–1) in vitro release test (ivrt) Pharmacy and materia medica RS1-441 Elena Bezuglaya Hanna Ivashchenko Nikolay Lyapunov Igor Zinchenko Anna Liapunova Yurij Stolper Oleksii Liapunov Tetiana Pukhova Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
description	The aim of our study was to identify factors affecting the in vitro release of diclofenac sodium (DS) from hypromellose-based gels (HPMC). Materials and methods. Gels with HPMC and liquids without HPMC were studied by viscosity-rotating viscometer method and spin probe electron paramagnetic resonance spectroscopy. Rheograms were used to determine the flow behavior and the apparent viscosity, and the EPR spectra were used to determine the rotational correlation time (τ–1) of the dissolved spin probes. The in vitro release tests were performed using vertical diffusion cells according to a validated procedure. The assay of DS and isopropyl alcohol (IPA) in the receptor medium was performed by high performance liquid chromatography (HPLC) and gas chromatography (GC) according to validated procedures, and the water content was determined using semi-micro method. Results. The apparent viscosity of the gels increased with increasing HPMC content and depended on the HPMC grade. The high apparent viscosity of the gels did not affect the values of τ–1 of the dissolved spin probes. In viscous gels and Newtonian fluids, the composition of which corresponded to the dispersion medium of gels, the values of τ–1 were identical and were in the range of rapid rotation, which is a prerequisite for similar and rapid release of the dissolved substances from gels and liquids. It was shown that the HPMC-based gel and Newtonian liquid without HPMC in terms of in vitro release parameters DS and IPA were equivalent. During in vitro testing the release of dissolved DS increased with increasing its concentration in the gel and depended on the dispersed state of DS. When the content of IPA was changed from 45.0 % to 22.5 %, the water absorption by the gel and the release of IPA decreased, and the release of DS increased, which was due to the decrease in the solubility of DS in the gel. Conclusions. HPMC, which provided high apparent viscosity of the gels, did not affect the value of τ–1 of the dissolved spin probes and the in vitro release of DS from the gels. The gel and Newtonian liquid were equivalent in terms of in vitro release of DS and IPA. The release of DS altered proportionally with the concentration of DS and depended on its dispersed state. As the content of IPA decreased, the release of IPA decreased, but the release of DS increased because of the decrease in the solubility of the DS in the gel
format	article
author	Elena Bezuglaya Hanna Ivashchenko Nikolay Lyapunov Igor Zinchenko Anna Liapunova Yurij Stolper Oleksii Liapunov Tetiana Pukhova
author_facet	Elena Bezuglaya Hanna Ivashchenko Nikolay Lyapunov Igor Zinchenko Anna Liapunova Yurij Stolper Oleksii Liapunov Tetiana Pukhova
author_sort	Elena Bezuglaya
title	Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
title_short	Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
title_full	Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
title_fullStr	Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
title_full_unstemmed	Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
title_sort	study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels
publisher	PC Technology Center
publishDate	2021
url	https://doaj.org/article/5eeae36c2b114ddd9a55884a31867287
work_keys_str_mv	AT elenabezuglaya studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT hannaivashchenko studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT nikolaylyapunov studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT igorzinchenko studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT annaliapunova studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT yurijstolper studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT oleksiiliapunov studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels AT tetianapukhova studyoffactorsaffectingtheinvitroreleaseofdiclofenacsodiumfromhypromelosebasedgels
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Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels

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