Cargando…
Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain
1,4-Dihydropyridines (DHPs) are the most important class of L-type calcium channel blockers that are employed for the treatment of cardiovascular diseases, particularly hypertension. Various modifications on this scaffold lead to the discovery of new DHPs blocking different types of calcium channels...
Autores principales: | , , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070562/ https://www.ncbi.nlm.nih.gov/pubmed/33920090 http://dx.doi.org/10.3390/pharmaceutics13040527 |
_version_ | 1783683499135336448 |
---|---|
author | Ioele, Giuseppina Muzzalupo, Rita Gündüz, Miyase Gözde De Luca, Michele Mazzotta, Elisabetta Grande, Fedora Occhiuzzi, Maria Antonietta Garofalo, Antonio Ragno, Gaetano |
author_facet | Ioele, Giuseppina Muzzalupo, Rita Gündüz, Miyase Gözde De Luca, Michele Mazzotta, Elisabetta Grande, Fedora Occhiuzzi, Maria Antonietta Garofalo, Antonio Ragno, Gaetano |
author_sort | Ioele, Giuseppina |
collection | PubMed |
description | 1,4-Dihydropyridines (DHPs) are the most important class of L-type calcium channel blockers that are employed for the treatment of cardiovascular diseases, particularly hypertension. Various modifications on this scaffold lead to the discovery of new DHPs blocking different types of calcium channels. Among them, the T-type calcium channel has recently attracted great interest due to its role in chronic pain conditions. In this study, we selected three newly synthesized DHPs (HM8, HM10 and MD20) with different selectivity profiles to the T-type calcium channel and formulated them in micellar solutions and micellar-in-gel matrices to be tested for potential topical use in the treatment of neuropathic pain. To prevent the well-known sensitivity to light of the DHPs, the studied compounds were entrapped in colloidal aggregates obtained by using edible Pluronic(®) surfactants and adding α-tocopherol as an antioxidant. All the prepared formulations were exposed to stressing light, according to international rules. Along with the degradation experiments, the concentrations of the parent compounds and by-products were calculated by multivariate curve resolution—alternating least squares (MCR-ALS) applied to the spectral data. The defined formulations proved suitable as light-stable matrices for the DHP compounds, showing an increase in stability for HM8 and MD20 and an almost complete photoprotection for HM10, compared to ethanol solutions and standard gel formulations. |
format | Online Article Text |
id | pubmed-8070562 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-80705622021-04-26 Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain Ioele, Giuseppina Muzzalupo, Rita Gündüz, Miyase Gözde De Luca, Michele Mazzotta, Elisabetta Grande, Fedora Occhiuzzi, Maria Antonietta Garofalo, Antonio Ragno, Gaetano Pharmaceutics Article 1,4-Dihydropyridines (DHPs) are the most important class of L-type calcium channel blockers that are employed for the treatment of cardiovascular diseases, particularly hypertension. Various modifications on this scaffold lead to the discovery of new DHPs blocking different types of calcium channels. Among them, the T-type calcium channel has recently attracted great interest due to its role in chronic pain conditions. In this study, we selected three newly synthesized DHPs (HM8, HM10 and MD20) with different selectivity profiles to the T-type calcium channel and formulated them in micellar solutions and micellar-in-gel matrices to be tested for potential topical use in the treatment of neuropathic pain. To prevent the well-known sensitivity to light of the DHPs, the studied compounds were entrapped in colloidal aggregates obtained by using edible Pluronic(®) surfactants and adding α-tocopherol as an antioxidant. All the prepared formulations were exposed to stressing light, according to international rules. Along with the degradation experiments, the concentrations of the parent compounds and by-products were calculated by multivariate curve resolution—alternating least squares (MCR-ALS) applied to the spectral data. The defined formulations proved suitable as light-stable matrices for the DHP compounds, showing an increase in stability for HM8 and MD20 and an almost complete photoprotection for HM10, compared to ethanol solutions and standard gel formulations. MDPI 2021-04-10 /pmc/articles/PMC8070562/ /pubmed/33920090 http://dx.doi.org/10.3390/pharmaceutics13040527 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 Ioele, Giuseppina Muzzalupo, Rita Gündüz, Miyase Gözde De Luca, Michele Mazzotta, Elisabetta Grande, Fedora Occhiuzzi, Maria Antonietta Garofalo, Antonio Ragno, Gaetano Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title | Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title_full | Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title_fullStr | Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title_full_unstemmed | Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title_short | Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain |
title_sort | use of pluronic surfactants in gel formulations of photosensitive 1,4-dihydropyridine derivatives: a potential approach in the treatment of neuropathic pain |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070562/ https://www.ncbi.nlm.nih.gov/pubmed/33920090 http://dx.doi.org/10.3390/pharmaceutics13040527 |
work_keys_str_mv | AT ioelegiuseppina useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT muzzaluporita useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT gunduzmiyasegozde useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT delucamichele useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT mazzottaelisabetta useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT grandefedora useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT occhiuzzimariaantonietta useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT garofaloantonio useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain AT ragnogaetano useofpluronicsurfactantsingelformulationsofphotosensitive14dihydropyridinederivativesapotentialapproachinthetreatmentofneuropathicpain |