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Co-hybridized composite nanovesicles for enhanced transdermal eugenol and cinnamaldehyde delivery and their potential efficacy in ulcerative colitis.
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 5.4 ) Pub Date : 2020-04-22 , DOI: 10.1016/j.nano.2020.102212
Yongtai Zhang 1 , Hongyu Zhang 1 , Kai Zhang 1 , Zhe Li 1 , Teng Guo 1 , Tong Wu 1 , Xuefeng Hou 1 , Nianping Feng 1
Affiliation  

Percutaneous absorption of drugs can be enhanced by ethosomes, which are nanocarriers with excellent deformability and drug-loading properties. However, the ethanol within ethosomes increases phospholipid membrane fluidity and permeability, leading to drug leakage during storage. Here, we developed and characterized a new phospholipid nanovesicles that is co-hybridized with hyaluronic acid (HA), ethanol and the encapsulated volatile oil medicines (eugenol and cinnamaldehyde [EUG/CAH]) for transdermal administration. In comparison with EUG/CAH-loaded ethosomes (ES), the formulation stability and percutaneous drug absorption of EUG/CAH-loaded HA-immobilized ethosomes (HA-ES) were significantly improved. After transdermal administration of HA-ES, the interstitial cells of Cajal in the colon of rats with trinitrobenzene sulfonate-induced ulcerative colitis (UC) were significantly increased, and the stem cell factor/c-kit signaling pathway was partly repaired. Overall, HA-ES possesses excellent deformability and showed improved efficacy against UC compared with ES, which is demonstrated as a promising transdermal delivery vehicle for volatile oil medicines.

中文翻译:

共杂交复合纳米囊泡,用于增强透皮丁香酚和肉桂醛的递送及其在溃疡性结肠炎中的潜在功效。

脂质体可以增强药物的经皮吸收,而脂质体是具有优异的可变形性和载药性的纳米载体。但是,乙醇中的乙醇会增加磷脂膜的流动性和渗透性,从而导致药物在储存过程中泄漏。在这里,我们开发并鉴定了一种新的磷脂纳米囊泡,可与透明质酸(HA),乙醇和包封的挥发油药物(丁香酚和肉桂醛[EUG / CAH])共混和用于经皮给药。与载有EUG / CAH的核糖体(ES)相比,EUG / CAH载有HA的固定体(HA-ES)的制剂稳定性和经皮药物吸收得到了显着改善。经皮给予HA-ES后,三硝基苯磺酸盐诱导的溃疡性结肠炎(UC)大鼠结肠中Cajal的间质细胞显着增加,并且干细胞因子/ c-kit信号通路得以部分修复。总体而言,与ES相比,HA-ES具有出色的可变形性,并且对UC表现出更高的功效,这被证明是一种很有前景的挥发油药物透皮给药载体。
更新日期:2020-04-22
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