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姜黄素经皮给药增强传递用于斑块状银屑病的有效治疗:设计、配方、特性描述和体内研究。

Augmented Transdermal Delivery of Curcumin for the Effective Management of Plaque Psoriasis - Design, Formulation, Characterisation, and In Vivo Studies.

机构信息

Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, Delhi Pharmaceutical Sciences and Research University (DPSRU) Pushp Vihar Sector III, MB Road, New Delhi, 110017, India.

出版信息

AAPS PharmSciTech. 2023 Jun 8;24(5):134. doi: 10.1208/s12249-023-02595-8.

Abstract

Psoriasis is a recurrent, life-threatening anti-inflammatory condition that affects nearly 1-3% of the global population. It is an autoimmune illness distinguished by hyperplasia of skin cells or fast skin cell development, resulting in abnormally irritating scales and skin patches. Curcumin, as a selective phosphorylase kinase inhibitor, actively suppresses inflammation and keratinocyte proliferation in psoriasis. However, limited solubility in water and poor skin permeability poses a significant hurdle in curcumin's topical effectiveness in psoriasis. The present study focuses on enhancing the solubility and skin permeability of curcumin for better transdermal application. Curcumin-loaded invasomes were formulated, and a factorial design was applied to study the effect of the type of terpenes and their concentrations on the properties of prepared invasomes. A topical gel was formulated using the optimised invasomal formulation which was further evaluated for anti-psoriatic potential in BALB/c mice. The optimised formulation showed 85.84 ± 0.56% entrapment efficiency and a vesicle size of 302.33 ± 1.53 nm. The invasomal gel of the optimised formulation showed a permeation flux of 3 times greater than the plain gel. In vivo studies demonstrated that the invasomal gel of curcumin promoted faster and earlier recovery in psoriatic mice than conventional curcumin gel.

摘要

银屑病是一种反复发作、危及生命的炎症性疾病,影响全球近 1-3%的人口。它是一种自身免疫性疾病,其特征是皮肤细胞过度增生或快速皮肤细胞发育,导致异常刺激性鳞片和皮肤斑块。姜黄素作为一种选择性磷酸化酶激酶抑制剂,能积极抑制银屑病中的炎症和角质形成细胞增殖。然而,在水中的溶解度有限和皮肤渗透性差,这对姜黄素在银屑病中的局部疗效构成了重大障碍。本研究旨在提高姜黄素的溶解度和皮肤渗透性,以实现更好的经皮应用。制备了姜黄素包封的入侵囊泡,并应用析因设计研究了萜烯类型及其浓度对制备的入侵囊泡性质的影响。使用优化的入侵囊泡制剂制备了局部凝胶,并进一步在 BALB/c 小鼠中评估其抗银屑病潜力。优化的制剂显示出 85.84 ± 0.56%的包封效率和 302.33 ± 1.53nm 的囊泡大小。优化制剂的入侵囊泡凝胶的渗透通量比普通凝胶高 3 倍。体内研究表明,与普通姜黄素凝胶相比,姜黄素入侵囊泡凝胶能更快更早地促进银屑病小鼠的恢复。

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