配制和优化含有莱弗卢诺胺的NLC凝,以改善皮肤透性和抗炎疗效
Vivek Mewada1, Jigar Shah1, Aakash Kumar2
1Department of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, India.
Journal of drug targeting
|January 28, 2026
概括
这项研究开发了优化的 leflunomide-loaded 纳米结构脂质载体 (NLC) 用于局部关节炎治疗. 该NLC凝配方在体内表现出增强的皮肤透性和显著的抗炎作用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 关节炎需要有效的局部治疗关节炎症.
- 局部分娩为局部关节炎管理提供了一个有前途的途径.
- 莱弗卢诺胺是一种成熟的抗炎药物,但其局部应用需要优化的输送系统.
研究的目的:
- 为了制定和优化纳米结构的脂质载体 (NLCs) 用于局部输送.
- 使用设计质量原则系统优化NLC配方.
- 评估优化NLC基凝的物理化学特性,药物释放,皮肤透和体内抗炎疗效.
主要方法:
- 纳米结构脂质载体 (NLCs) 通过高速同质化和探头声学来制定.
- 为了参数选和优化,采用了双重实验设计 (Plackett-Burman和Box-Behnken).
- 物理化学表征包括粒子大小,PDI,泽塔潜力,捕获效率,DSC,P-XRD和TEM.
- 优化的NLC被纳入卡博波尔凝中,并评估了其风湿性质,药物释放和ex vivo皮肤透.
- 在体内对抗炎症活性进行了评估,使用卡拉基南诱导的脚胀模型.
主要成果:
- 优化的NLCs的粒子大小为125.5nm,PDI为0.188,泽塔电位为-15.5mV,捕获效率高 (92.20%).
- 鉴定证实了Leflunomide在脂质矩阵和球形NLC形态中的无形分散.
- 基于NLC的凝显示出有利的风湿性质,持续的药物释放 (在24小时内96%),以及增强的ex vivo皮肤透 (流量为0.3632mg/cm2/h).
- 在体内研究表明,炎症减少了89.40%,超过了市场上的配方.
结论:
- 通过设计的质量方法成功地优化了含有莱夫卢诺胺的NLC用于局部输送.
- 基于NLC的凝配方提供了增强的皮肤透和持续的药物释放.
- 这种含有勒诺胺的NLC凝代表了有效的局部治疗关节炎的有希望的平台,具有改善的抗炎活性.
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