Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System

Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, wer...

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Autores principales: Grande, Fedora, Ragno, Gaetano, Muzzalupo, Rita, Occhiuzzi, Maria Antonietta, Mazzotta, Elisabetta, De Luca, Michele, Garofalo, Antonio, Ioele, Giuseppina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7284650/
https://www.ncbi.nlm.nih.gov/pubmed/32380748
http://dx.doi.org/10.3390/pharmaceutics12050423
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author Grande, Fedora
Ragno, Gaetano
Muzzalupo, Rita
Occhiuzzi, Maria Antonietta
Mazzotta, Elisabetta
De Luca, Michele
Garofalo, Antonio
Ioele, Giuseppina
author_facet Grande, Fedora
Ragno, Gaetano
Muzzalupo, Rita
Occhiuzzi, Maria Antonietta
Mazzotta, Elisabetta
De Luca, Michele
Garofalo, Antonio
Ioele, Giuseppina
author_sort Grande, Fedora
collection PubMed
description Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical gel formulations of both compounds. The photodegradation profiles were monitored by Multivariate curve resolution applied to the UV spectral data. The inclusion of the compounds in microemulsion was investigated to improve light stability and, at the same time, to ensure a sustained release system for skin delivery. All the formulations in solution, gel, microemulsion, and microemulsion-in-gel were exposed to a forced irradiation of 350 W/m(2), corresponding to a 21 kJ/m(2) min, for up to 300 min. Photostability increased significantly for both drugs in the liquid microemulsion and microemulsion-in-gel, compared to the ethanol solution and plain gel, reaching a residual drug of 97% and 98% for Nabumetone and analog in microemulsion-in-gel, respectively. Permeation experiments on the microemulsion-in-gel showed a better performance of the analog formulated at 0.2%, compared to the same formulation of Nabumetone at 0.7%. These results highlight the potential of the designed matrices as delayed drug delivery systems along with the use of lower drug doses leading to reduced side effects.
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spelling pubmed-72846502020-06-15 Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System Grande, Fedora Ragno, Gaetano Muzzalupo, Rita Occhiuzzi, Maria Antonietta Mazzotta, Elisabetta De Luca, Michele Garofalo, Antonio Ioele, Giuseppina Pharmaceutics Article Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical gel formulations of both compounds. The photodegradation profiles were monitored by Multivariate curve resolution applied to the UV spectral data. The inclusion of the compounds in microemulsion was investigated to improve light stability and, at the same time, to ensure a sustained release system for skin delivery. All the formulations in solution, gel, microemulsion, and microemulsion-in-gel were exposed to a forced irradiation of 350 W/m(2), corresponding to a 21 kJ/m(2) min, for up to 300 min. Photostability increased significantly for both drugs in the liquid microemulsion and microemulsion-in-gel, compared to the ethanol solution and plain gel, reaching a residual drug of 97% and 98% for Nabumetone and analog in microemulsion-in-gel, respectively. Permeation experiments on the microemulsion-in-gel showed a better performance of the analog formulated at 0.2%, compared to the same formulation of Nabumetone at 0.7%. These results highlight the potential of the designed matrices as delayed drug delivery systems along with the use of lower drug doses leading to reduced side effects. MDPI 2020-05-05 /pmc/articles/PMC7284650/ /pubmed/32380748 http://dx.doi.org/10.3390/pharmaceutics12050423 Text en © 2020 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Grande, Fedora
Ragno, Gaetano
Muzzalupo, Rita
Occhiuzzi, Maria Antonietta
Mazzotta, Elisabetta
De Luca, Michele
Garofalo, Antonio
Ioele, Giuseppina
Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title_full Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title_fullStr Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title_full_unstemmed Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title_short Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
title_sort gel formulation of nabumetone and a newly synthesized analog: microemulsion as a photoprotective topical delivery system
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7284650/
https://www.ncbi.nlm.nih.gov/pubmed/32380748
http://dx.doi.org/10.3390/pharmaceutics12050423
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