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新型纳米乳凝胶含姜黄素、百里醌和白藜芦醇三重天然生物活性成分,改善银屑病治疗:体外和体内研究。

Novel nanoemulsion gel containing triple natural bio-actives combination of curcumin, thymoquinone, and resveratrol improves psoriasis therapy: in vitro and in vivo studies.

机构信息

Nanomedicine Research Lab, Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India.

Department of Biosciences, Jamia Millia Islamia, New Delhi, India.

出版信息

Drug Deliv Transl Res. 2021 Jun;11(3):1245-1260. doi: 10.1007/s13346-020-00852-y. Epub 2020 Sep 23.

Abstract

Curcumin, resveratrol, and thymoquinone are the potential natural bio-actives reported with good anti-psoriatic activity. However, poor aqueous solubility and limited skin permeation of these natural bio-actives hinder their effective delivery and potential therapeutic outcome. In this regard, current research work focuses on the design and optimization of nanoemulsion (NE) gel formulation for the concurrent delivery of these three drugs. The NE system is consisting of oleic acid as oil phase, Tween 20 as surfactant, and PEG 200 as co-surfactant. The optimized formulation exhibited the droplet size 76.20 ± 1.67 nm, PDI of 0.12 ± 0.05, RI of 1.403 ± 0.007, and viscosity of 137.9 ± 4.07 mp. Carbopol 940 (0.5% w/v) was used as the gelling agent to prepare the NE gel which exhibited a good texture profile. The optimized formulation exhibited a higher % of growth inhibition on A-431 cells and demonstrated good anti-angiogenic activity in the HET-CAM test. Finally, in vivo studies in Balb/c mice model showed improved anti-psoriatic conditions which indicated that the triple natural bio-actives combination in nanoemulgel formulation is effective in the management of psoriasis.

摘要

姜黄素、白藜芦醇和百里醌是具有良好抗银屑病活性的潜在天然生物活性物质。然而,这些天然生物活性物质的水溶性差和皮肤渗透性有限,阻碍了它们的有效传递和潜在的治疗效果。在这方面,目前的研究工作集中在设计和优化纳米乳 (NE) 凝胶制剂,以同时输送这三种药物。该 NE 系统由油酸作为油相、吐温 20 作为表面活性剂和 PEG 200 作为助表面活性剂组成。优化后的配方表现出的粒径为 76.20 ± 1.67nm、PDI 为 0.12 ± 0.05、RI 为 1.403 ± 0.007 和粘度为 137.9 ± 4.07mp。Carbopol 940(0.5%w/v)用作凝胶剂来制备 NE 凝胶,其表现出良好的质地轮廓。优化后的配方对 A-431 细胞的生长抑制率更高,并在 HET-CAM 试验中表现出良好的抗血管生成活性。最后,在 Balb/c 小鼠模型中的体内研究表明改善了银屑病状况,这表明纳米乳凝胶制剂中的三种天然生物活性物质组合在治疗银屑病方面是有效的。

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