Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation

Arthritic disease is one of the most common diseases in adults and a leading cause of joint degeneration. Dexibuprofen (DEX) is routinely used for the treatment of rheumatoid arthritis, acute postoperative pain, primary dysmenorrheal, and in lower back pain. However, it is poorly water soluble with...

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Published in:Colloids and Surfaces B: Biointerfaces
Main Author: Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
Format: Article
Language:English
Published: Elsevier B.V. 2025
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85210372378&doi=10.1016%2fj.colsurfb.2024.114407&partnerID=40&md5=c857d9e3e9e4af9d228e74740e74d8ad
id 2-s2.0-85210372378
spelling 2-s2.0-85210372378
Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
2025
Colloids and Surfaces B: Biointerfaces
247

10.1016/j.colsurfb.2024.114407
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85210372378&doi=10.1016%2fj.colsurfb.2024.114407&partnerID=40&md5=c857d9e3e9e4af9d228e74740e74d8ad
Arthritic disease is one of the most common diseases in adults and a leading cause of joint degeneration. Dexibuprofen (DEX) is routinely used for the treatment of rheumatoid arthritis, acute postoperative pain, primary dysmenorrheal, and in lower back pain. However, it is poorly water soluble with compromised bioavailability, and hence has limited therapeutic activity. In order to overcome these issues, we studied the formulation and characterization of nanoemulsion based system i.e nanoemulgel of DEX. This study aimed to prepare topical nanoemulgel containing 2 % DEX and solubility-enhanced DEX via ternary inclusion complexation (DEX-SE-T) and to compare it with commercially available 5 % Ibuprofen gel as there is no topical formulation of DEX is available in the market currently. A pseudoternary phase diagram was constructed using the spontaneous water titration method. Blank and drug-loaded nanoemulgel were prepared using a high-speed homogenization method. All the formulations were evaluated in terms of particle size, pH, conductivity, viscosity, zeta potential, and ex vivo drug permeation. DEX loaded nanoemulgel yield enhanced in vitro skin permeation than the commercially available 5 % ibuprofen gel. The optimized nanoemulgel formulation (DEX-SE-T) was tested in in vivo anti-inflammatory models including cotton pellets-induced abdominal granuloma (chronic inflammation) and carrageenan-induced paw edema (acute inflammation). DEX-SE-T loaded nanoemulgel has improved in vivo anti-inflammatory activity as compared to ibuprofen gel. DEX-SE-T could be a promising option for effective topical treatment of inflammatory conditions. © 2024 Elsevier B.V.
Elsevier B.V.
09277765
English
Article

author Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
spellingShingle Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
author_facet Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
author_sort Munir R.; Khan I.U.; Kamal Y.; Asghar S.; Irfan M.; Alshammari A.; Asif M.; Albekairi N.A.; Shah P.A.; Khalid I.; Munir M.R.; Khalid S.H.
title Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
title_short Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
title_full Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
title_fullStr Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
title_full_unstemmed Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
title_sort Dexibuprofen loaded into nanoemulsion based gel for topical application – In vitro characterization and in vivo anti-inflammatory evaluation
publishDate 2025
container_title Colloids and Surfaces B: Biointerfaces
container_volume 247
container_issue
doi_str_mv 10.1016/j.colsurfb.2024.114407
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85210372378&doi=10.1016%2fj.colsurfb.2024.114407&partnerID=40&md5=c857d9e3e9e4af9d228e74740e74d8ad
description Arthritic disease is one of the most common diseases in adults and a leading cause of joint degeneration. Dexibuprofen (DEX) is routinely used for the treatment of rheumatoid arthritis, acute postoperative pain, primary dysmenorrheal, and in lower back pain. However, it is poorly water soluble with compromised bioavailability, and hence has limited therapeutic activity. In order to overcome these issues, we studied the formulation and characterization of nanoemulsion based system i.e nanoemulgel of DEX. This study aimed to prepare topical nanoemulgel containing 2 % DEX and solubility-enhanced DEX via ternary inclusion complexation (DEX-SE-T) and to compare it with commercially available 5 % Ibuprofen gel as there is no topical formulation of DEX is available in the market currently. A pseudoternary phase diagram was constructed using the spontaneous water titration method. Blank and drug-loaded nanoemulgel were prepared using a high-speed homogenization method. All the formulations were evaluated in terms of particle size, pH, conductivity, viscosity, zeta potential, and ex vivo drug permeation. DEX loaded nanoemulgel yield enhanced in vitro skin permeation than the commercially available 5 % ibuprofen gel. The optimized nanoemulgel formulation (DEX-SE-T) was tested in in vivo anti-inflammatory models including cotton pellets-induced abdominal granuloma (chronic inflammation) and carrageenan-induced paw edema (acute inflammation). DEX-SE-T loaded nanoemulgel has improved in vivo anti-inflammatory activity as compared to ibuprofen gel. DEX-SE-T could be a promising option for effective topical treatment of inflammatory conditions. © 2024 Elsevier B.V.
publisher Elsevier B.V.
issn 09277765
language English
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