Cargando…

Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect

BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers t...

Descripción completa

Detalles Bibliográficos
Autores principales: Pető, Ágota, Kósa, Dóra, Haimhoffer, Ádám, Fehér, Pálma, Ujhelyi, Zoltán, Sinka, Dávid, Fenyvesi, Ferenc, Váradi, Judit, Vecsernyés, Miklós, Gyöngyösi, Alexandra, Lekli, István, Szentesi, Péter, Marton, Annamária, Gombos, Imre, Dukic, Barbara, Vígh, László, Bácskay, Ildikó
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707203/
https://www.ncbi.nlm.nih.gov/pubmed/34959318
http://dx.doi.org/10.3390/pharmaceutics13122037
_version_ 1784622379555618816
author Pető, Ágota
Kósa, Dóra
Haimhoffer, Ádám
Fehér, Pálma
Ujhelyi, Zoltán
Sinka, Dávid
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Gyöngyösi, Alexandra
Lekli, István
Szentesi, Péter
Marton, Annamária
Gombos, Imre
Dukic, Barbara
Vígh, László
Bácskay, Ildikó
author_facet Pető, Ágota
Kósa, Dóra
Haimhoffer, Ádám
Fehér, Pálma
Ujhelyi, Zoltán
Sinka, Dávid
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Gyöngyösi, Alexandra
Lekli, István
Szentesi, Péter
Marton, Annamária
Gombos, Imre
Dukic, Barbara
Vígh, László
Bácskay, Ildikó
author_sort Pető, Ágota
collection PubMed
description BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers to ensure good drug delivery, improve bioavailability of the drug and investigate the potential anti-inflammatory effect of BGP-15 creams in vivo. Since the exact mechanism of the effect is still unknown, the antioxidant effect (tested with UVB radiation) and the ability of BGP-15 to decrease macrophage activation were evaluated. Biocompatibility investigations were carried out on HaCaT cells to make sure that the formulations and the selected excipients can be safely used. Dosage form studies were also completed with texture analysis and in vitro release with Franz diffusion chamber apparatus. Our results show that the ointments were able to reduce the extent of local inflammation in mice, but the exact mechanism of the effect remains unknown since BGP-15 did not show any antioxidant effect, nor was it able to decrease LPS-induced macrophage activation. Our results support the hypothesis that BGP-15 has a potential anti-inflammatory effect, even if it is topically applied, but the mechanism of the effect remains unclear and requires further pharmacological studies.
format Online
Article
Text
id pubmed-8707203
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-87072032021-12-25 Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect Pető, Ágota Kósa, Dóra Haimhoffer, Ádám Fehér, Pálma Ujhelyi, Zoltán Sinka, Dávid Fenyvesi, Ferenc Váradi, Judit Vecsernyés, Miklós Gyöngyösi, Alexandra Lekli, István Szentesi, Péter Marton, Annamária Gombos, Imre Dukic, Barbara Vígh, László Bácskay, Ildikó Pharmaceutics Article BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers to ensure good drug delivery, improve bioavailability of the drug and investigate the potential anti-inflammatory effect of BGP-15 creams in vivo. Since the exact mechanism of the effect is still unknown, the antioxidant effect (tested with UVB radiation) and the ability of BGP-15 to decrease macrophage activation were evaluated. Biocompatibility investigations were carried out on HaCaT cells to make sure that the formulations and the selected excipients can be safely used. Dosage form studies were also completed with texture analysis and in vitro release with Franz diffusion chamber apparatus. Our results show that the ointments were able to reduce the extent of local inflammation in mice, but the exact mechanism of the effect remains unknown since BGP-15 did not show any antioxidant effect, nor was it able to decrease LPS-induced macrophage activation. Our results support the hypothesis that BGP-15 has a potential anti-inflammatory effect, even if it is topically applied, but the mechanism of the effect remains unclear and requires further pharmacological studies. MDPI 2021-11-29 /pmc/articles/PMC8707203/ /pubmed/34959318 http://dx.doi.org/10.3390/pharmaceutics13122037 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pető, Ágota
Kósa, Dóra
Haimhoffer, Ádám
Fehér, Pálma
Ujhelyi, Zoltán
Sinka, Dávid
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Gyöngyösi, Alexandra
Lekli, István
Szentesi, Péter
Marton, Annamária
Gombos, Imre
Dukic, Barbara
Vígh, László
Bácskay, Ildikó
Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title_full Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title_fullStr Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title_full_unstemmed Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title_short Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect
title_sort nicotinic amidoxime derivate bgp-15, topical dosage formulation and anti-inflammatory effect
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707203/
https://www.ncbi.nlm.nih.gov/pubmed/34959318
http://dx.doi.org/10.3390/pharmaceutics13122037
work_keys_str_mv AT petoagota nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT kosadora nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT haimhofferadam nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT feherpalma nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT ujhelyizoltan nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT sinkadavid nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT fenyvesiferenc nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT varadijudit nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT vecsernyesmiklos nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT gyongyosialexandra nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT lekliistvan nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT szentesipeter nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT martonannamaria nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT gombosimre nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT dukicbarbara nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT vighlaszlo nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect
AT bacskayildiko nicotinicamidoximederivatebgp15topicaldosageformulationandantiinflammatoryeffect