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脂质体介导的透皮递送姜黄素治疗银屑病。

Liposphere mediated topical delivery of thymoquinone in the treatment of psoriasis.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.

Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.

出版信息

Nanomedicine. 2017 Oct;13(7):2251-2262. doi: 10.1016/j.nano.2017.06.009. Epub 2017 Jun 22.

Abstract

Thymoquinone (TMQ) is reported with good anti-psoriatic activity; however, the hydrophobicity, poor aqueous solubility, light and pH sensitive nature of TMQ hinder its delivery to target site. To address these delivery challenges of TMQ, lipospheres were explored. The topical use of lipospheres offers an effective mean of penetration along with stability and scalability. TMQ lipospheres of particle size below 70 nm were prepared and evaluated. These lipospheres resulted in deeper skin penetration, slow release and skin compatibility. Anti-inflammatory and anti-psoriatic potential of lipospheres was determined using in vitro cell lines and imiquimod induced psoriatic plaque model. Cell lines studies indicated reduction in the level of nitric oxide and IL-2, IL-6, IL-1β, TNF-α, whereas in vivo results indicated improvement in the phenotypic, histopathological features and reduced level of IL-17 and TNF-α in psoriatic skin. These results suggest the potential of TMQ lipospheres in the management of psoriasis.

摘要

姜黄色素(TMQ)具有良好的抗银屑病活性;然而,TMQ 的疏水性、低水溶性、对光和 pH 敏感的性质阻碍了其递送到靶部位。为了解决 TMQ 的这些递药难题,人们探索了脂质体。脂质体的局部应用提供了一种有效的渗透手段,同时具有稳定性和可扩展性。制备并评价了粒径低于 70nm 的 TMQ 脂质体。这些脂质体导致更深的皮肤渗透、缓慢释放和皮肤相容性。使用体外细胞系和咪喹莫特诱导的银屑病斑块模型来确定脂质体的抗炎和抗银屑病潜力。细胞系研究表明,NO 和 IL-2、IL-6、IL-1β、TNF-α 的水平降低,而体内结果表明,银屑病皮肤中 IL-17 和 TNF-α 的表型、组织病理学特征和水平降低。这些结果表明 TMQ 脂质体在银屑病治疗中的潜力。

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