磷酸鲁索利替尼外用纳米脂质体制剂的设计

Q4 Pharmacology, Toxicology and Pharmaceutics
Atefeh Naeimifar, S. Ahmad Nasrollahi, H. Akbari Javar, Mansoor Nassiri Kashani, A. Firooz, M. Rouini
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引用次数: 1

摘要

背景:JAK-STAT通路在自身免疫性皮肤病的免疫反应失调中起着至关重要的作用。Ruxolitinib是JAK1和JAK2的选择性抑制剂,可有效抑制细胞因子信号传导。方法:采用薄膜水合法制备鲁索利替尼纳米脂质体外用凝胶。在25±2℃/60±5% RH条件下,观察其12个月的理化特性。根据颗粒特性、扫描电镜(SEM)、包封效率(EE)、载药量(DL)和差示扫描量热法(DSC)对RuxoLip进行评估。对乳状液进行pH、密度、粘度、微生物评价、体外释药及体内胶带剥离试验。采用紫外光谱法对分析方法进行验证。结果:制备的纳米脂质体具有良好的粒径(218±2 nm), EE为67%,DL为8%。该制剂长期稳定。扫描电镜显示脂质体具有规则的球形表面。体外释药试验和体内贴剥试验均显示其具有良好的吸收和渗透作用。结论:脂质体剂型有望成为鲁索利替尼局部给药系统治疗自身免疫性皮肤病的理想载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Designing a Topical Nanoliposomal Formulation of Ruxolitinib Phosphate
Background: The JAK-STAT pathway has been revealed to play a crucial role in the dysregulation of immune responses in autoimmune skin disorders. Ruxolitinib, a selective inhibitor of JAK1 and JAK2, potently suppresses cytokine signaling. Methods: A topical emulgel containing ruxolitinib nanoliposome (RuxoLip) was prepared by thin film hydration method. Then, its physicochemical characteristics were evaluated at 25±2 ̊C/60±5% RH for 12 months. RuxoLip was assessed based on particle characteristics, Scanning Electron Microscopy (SEM), entrapment efficiency (EE), drug loading (DL), and Differential Scanning Calorimetry (DSC). The pH, density, viscosity, microbial assessment, in vitro drug release, and in vivo tape stripping test were evaluated on the emulgel of RuxoLip. Validating the analysis method was performed by UV spectroscopy. Results: Nanoliposomal preparation was successfully formulated with a good particle size (218±2 nm), an EE of 67% and a DL of 8%. The formulation was stable in a long-term condition. SEM showed that liposomes had a regular spherical surface. Moreover, in vitro drug release and the in vivo tape stripping test revealed good absorption and permeation, respectively. Conclusion: The liposome dosage form is anticipated to be a perfect carrier for the topical drug delivery system of ruxolitinib in autoimmune skin disorders.
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来源期刊
CiteScore
0.10
自引率
0.00%
发文量
17
审稿时长
10 weeks
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