Nanoemulgel, an Innovative Carrier for Diflunisal Topical Delivery with Profound Anti-Inflammatory Effect: in vitro and in vivo Evaluation.
Administration, Topical
Animals
Anti-Inflammatory Agents
/ pharmacology
Carrageenan
Diflunisal
/ administration & dosage
Disease Models, Animal
Drug Compounding
Drug Delivery Systems
Drug Liberation
Edema
/ drug therapy
Electric Conductivity
Emulsions
/ chemistry
Hydrogen-Ion Concentration
Male
Nanogels
/ chemistry
Particle Size
Permeability
Phase Transition
Polyethylene Glycols
/ chemistry
Polyethyleneimine
/ chemistry
Rats
Skin
/ drug effects
Skin Absorption
/ drug effects
Solubility
Surface-Active Agents
/ chemistry
Viscosity
anti-inflammatory activity
diflunisal
improved efficacy
in vitro skin permeation
nanoemulsion
pseudoternary phase diagram
Journal
International journal of nanomedicine
ISSN: 1178-2013
Titre abrégé: Int J Nanomedicine
Pays: New Zealand
ID NLM: 101263847
Informations de publication
Date de publication:
2021
2021
Historique:
received:
02
12
2020
accepted:
28
01
2021
entrez:
3
3
2021
pubmed:
4
3
2021
medline:
13
3
2021
Statut:
epublish
Résumé
Rheumatoid arthritis is an autoimmune disorder that directly affects joints. However, other body organs including heart, eyes, skin, blood vessels and lungs may also be affected. The purpose of this study was to design and evaluate a nanoemulgel formulation of diflunisal (DIF) and solubility enhanced diflunisal (DIF-IC) for enhanced topical anti-inflammatory activity. Nanoemulsion formulations of both DIF and DIF-IC were prepared and incorporated in three different gelling agents, namely carboxymethylcellulose sodium (CMC-Na), sodium alginate (Na-ALG) and xanthan gum (XG). All the formulations were evaluated in term of particle size, pH, conductivity, viscosity, zeta potential and in vitro drug release. The formulation 2 (NE2) of both DIF and DIF-IC which expressed optimum release and satisfactory physicochemical properties was incorporated with gelling agents to produce final nanoemulgel formulations. The optimized nanoemulgel formulation was subjected to three different in vivo anti-inflammatory models including carrageenan-induced paw edema model, histamine-induced paw edema model and formalin-induced paw edema model. DIF-IC-loaded nanoemulgel formulations yielded significantly enhanced in vitro skin permeation than DIF-loaded nanoemulgel. The nanoemulgel formulation of DIF-IC formulated with XG produced improved in vivo anti-inflammatory activity. It was recommended that DIF-IC-based nanoemulgel formulation prepared with XG could be a better option for effective topical treatment of inflammatory conditions.
Identifiants
pubmed: 33654396
doi: 10.2147/IJN.S294653
pii: 294653
pmc: PMC7910103
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Emulsions
0
Nanogels
0
Surface-Active Agents
0
polyethylene glycol polyethyleneimine nanogel
0
Polyethylene Glycols
3WJQ0SDW1A
Diflunisal
7C546U4DEN
Carrageenan
9000-07-1
Polyethyleneimine
9002-98-6
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1457-1472Informations de copyright
© 2021 Bashir et al.
Déclaration de conflit d'intérêts
The authors report that they have no conflicts of interest for this work.
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