Antipsoriatic Effect of Silymarin NLCs Based Gel: In Vitro and In Vivo Activity

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2024-08-21 DOI:10.1208/s12249-024-02910-x
Faijmahmad Momin, Vijay Kevlani, Shruti Rawal, Riya Patel, Sheetal Acharya, Shreeraj Shah
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Abstract

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 32 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.

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基于水飞蓟素 NLCs 的凝胶的抗银屑病效果:体外和体内活性
牛皮癣是一种慢性炎症性疾病,影响超过 1 亿人,需要长期治疗。目前的治疗方法只能缓解症状。然而,水飞蓟素(SLM)等基于植物成分的疗法已显示出良好的效果。本研究旨在开发、优化和评估一种新型稳定的水飞蓟素 NLC 凝胶,通过提高其在真皮层的渗透性和滞留性来改善抗银屑病活性。研究采用 32 种全因子设计制备和优化了 SLM NLC 配方。通过透射电子显微镜和热分析,对配方的粒度、PDI、ZETA电位和吸附效率进行了评估。对冷冻干燥和制备的 NLC 负载凝胶进行了理化参数、体外和体内研究评估。SLM负载的NLC粒径为624 nm,PDI为0.41,包埋效率为92.95%,ZETA电位为-31.6 mV。利用 TEM 技术确认了 NLC 的球形结构。在体内外研究中观察到药物的可控释放,与疾病对照组相比,PASI 评分较低。此外,IL-6、TNF-α 和 NF-κB 的水平也有所降低。组织病理学结果表明,SLM NLC 治疗组的角化不全现象极少,这也为上述结果提供了佐证。在体内研究中,制备的 NLC 可增强局部渗透性并减少银屑病斑块的厚度。
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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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