Department of Pharmaceutical Technology, L.J. Institute of Pharmacy, L J University, LJ Campus, Near Sarkhej-Sanand Circle, Off. S.G. Road, Ahmedabad, 382 210, India.
AAPS PharmSciTech. 2024 Aug 21;25(7):195. doi: 10.1208/s12249-024-02910-x.
Psoriasis is a chronic inflammatory disorder affecting over 100 million people, requires long-term therapy. Current treatments offer only symptomatic relief. However, phytoconstituents-based therapies like Silymarin (SLM) have shown promising effects. The study aims to develop, optimize, and evaluate a novel stable SLM NLC gel to improve anti-psoriatic activity by enhancing its permeability and retention into the dermal layer. SLM NLC formulation was prepared and optimized using 3 full factorial designs. The formulation was evaluated for the particle size, PDI, zeta potential, and % entrapment efficiency, evaluated by Transmission electron microscopy and thermal analysis. The freeze dried and prepared NLC-loaded gel was evaluated for physicochemical parameters, ex-vivo, and in-vivo studies. SLM-loaded NLC shows 624 nm particle size, 0.41 PDI, 92.95% entrapment efficiency, and -31.6 mV zeta potential. The sphere form of NLCs was confirmed using TEM. Controlled drug release was observed in ex vivo studies, low PASI score compared to disease control. Further, the levels of IL-6, TNF-α, and NF-κB were also reduced. The results are supported by histopathology showing minimal parakeratosis indicated in the SLM NLC-treated group. Prepared NLC-based shows enhance topical penetration and decrease the thickness of psoriatic plaques in the in vivo study.
银屑病是一种影响超过 1 亿人的慢性炎症性疾病，需要长期治疗。目前的治疗方法只能提供症状缓解。然而，基于植物成分的治疗方法，如水飞蓟素（SLM），已经显示出了有希望的效果。本研究旨在开发、优化和评估一种新型稳定的 SLM NLC 凝胶，通过增强其向真皮层的渗透性和滞留性来提高其抗银屑病活性。使用 3 因素完全设计法制备和优化了 SLM NLC 配方。通过透射电子显微镜和热分析评估了配方的粒径、PDI、zeta 电位和 %包封效率。对冻干和制备的 NLC 载药凝胶进行了理化参数、离体和体内研究的评价。SLM 负载的 NLC 显示出 624nm 的粒径、0.41 的 PDI、92.95%的包封效率和-31.6mV 的 zeta 电位。NLC 的球形成形式通过 TEM 得到了确认。在离体研究中观察到了控释药物释放，与疾病对照相比 PASI 评分较低。此外，IL-6、TNF-α 和 NF-κB 的水平也降低了。组织病理学显示 SLM NLC 治疗组角化不全最小，这一结果得到了支持。在体内研究中，制备的基于 NLC 的载药凝胶显示出增强的透皮渗透作用，并减少了银屑病斑块的厚度。
