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High payload dexamethasone palmitate-loaded solid lipid nanoparticles for enhanced anti-inflammatory effects in acute skin inflammation model
  • Bae, Yumi ;
  • Zeb, Alam ;
  • Choi, Ho Ik ;
  • Ryu, Jeong Su ;
  • Gul, Maleeha ;
  • Noh, Ha Yeon ;
  • Cho, Junho ;
  • Gil, Junkyung ;
  • Shah, Fawad Ali ;
  • Chang, Sun Young ;
  • Bae, Ok Nam ;
  • Kim, Jin Ki
Citations

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Publication Year
2024-09-01
Journal
Journal of Pharmaceutical Investigation
Publisher
Springer
Citation
Journal of Pharmaceutical Investigation, Vol.54 No.5, pp.617-629
Keyword
Anti-inflammatoryDexamethasoneDexamethasone palmitateEar edemaSkin inflammationSolid lipid nanoparticles
All Science Classification Codes (ASJC)
Pharmaceutical SciencePharmacology, Toxicology and Pharmaceutics (miscellaneous)
Abstract
Purpose: Dexamethasone palmitate (DXPL) is a lipophilic derivative of dexamethasone (DXM) used to overcome the low drug-loading capacity and immediate release characteristics of DXM from nanoparticles. In this study, we investigated the potential of DXPL-loaded solid lipid nanoparticles (DXPL-SLNs) to increase drug encapsulation efficiency, prolong drug release, and alleviate skin inflammation. Methods: DXPL-SLNs were prepared using the nano-emulsion template technique with trilaurin as a lipid matrix and Tween 20, Span 20, and Brij 58 as a surfactant mixture. The physicochemical properties of DXPL-SLNs were examined in terms of particle size, polydispersity index, zeta potential, encapsulation efficiency, loading capacity, morphology, and crystalline behavior. The in vitro release profile of DXM from the DXPL-SLNs incubated in mouse plasma was assessed using a plasma conversion assay. In vivo anti-inflammatory effects of topically applied DXPL-SLNs were evaluated in mice with 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-induced ear edema. Results: The optimized DXPL-SLNs (DXPL/trilaurin/Tween 20/Span 20/Brij 58:4/2/2/0.2/4, w/w ratio, respectively) displayed a mean particle size of 182.8 ± 2.7 nm with a very high drug loading capacity of 30.4%. DXPL-SLNs showed substantially prolonged drug release in mouse plasma compared to DXPL solution. Furthermore, DXPL-SLNs showed enhanced anti-inflammatory effects by efficiently reducing TPA-induced ear edema. Conclusion: These findings suggest that DXPL-SLNs have great potential as anti-inflammatory therapeutics against acute skin inflammation.
ISSN
2093-6214
Language
eng
URI
https://aurora.ajou.ac.kr/handle/2018.oak/34033
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85188112287&origin=inward
DOI
https://doi.org/10.1007/s40005-024-00674-x
Journal URL
https://www.springer.com/journal/40005
Type
Article
Funding
This work was supported by the Materials/Parts Technology Development Program (Development of industry process of a new hyaluronic acid, 200 Pa\u00b7s or more, of more than 20 times compared to the existing for sustained-release DDS, 1415184765, 20016715) funded by the Ministry of Trade, Industry and Energy (MOTIE, Korea).
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