High payload dexamethasone palmitate-loaded solid lipid nanoparticles for enhanced anti-inflammatory effects in acute skin inflammation model

Yumi Bae1, Alam Zeb2, Ho-Ik Choi1, Jeong-Su Ryu1, Maleeha Gul2, Ha-Yeon Noh1, Junho Cho1, Junkyung Gil1, Fawad Ali Shah3, Sun-Young Chang4, Ok-Nam Bae1, Jin-Ki Kim1
1College of Pharmacy, Institute of Pharmaceutical Sciences and Technology, Hanyang University ERICA, Ansan, Republic of Korea
2Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan
3Department of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia
4College of Pharmacy and Research Institute of Pharmaceutical Science and Technology (RIPST), Ajou University, Suwon, Republic of Korea

Tóm tắt

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. 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. 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. These findings suggest that DXPL-SLNs have great potential as anti-inflammatory therapeutics against acute skin inflammation.

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Tài liệu tham khảo

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