Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Nanomedicine. 2020 Aug;28:102212. doi: 10.1016/j.nano.2020.102212. Epub 2020 Apr 22.
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.
经皮给药时，醇质体能够增强药物的渗透性，醇质体作为具有优良变形性和载药性的纳米载体，能够提高药物的经皮渗透作用。但是，醇质体中的乙醇会增加磷脂膜的流动性和通透性，导致药物在储存过程中泄漏。在这里，我们开发并表征了一种新型的磷脂纳米囊泡，该纳米囊泡与透明质酸（HA）、乙醇和包封的挥发性油药物（丁香酚和肉桂醛[EUG/CAH]）共杂交，用于经皮给药。与负载 EUG/CAH 的醇质体（ES）相比，负载 EUG/CAH 的透明质酸固定醇质体（HA-ES）的制剂稳定性和经皮药物吸收得到了显著改善。经皮给予 HA-ES 后，三硝基苯磺酸诱导的溃疡性结肠炎（UC）大鼠结肠 Cajal 间质细胞明显增加，干细胞因子/c-kit 信号通路部分得到修复。总的来说，HA-ES 具有优良的变形性，与 ES 相比，对 UC 的疗效得到了改善，这表明它是一种有前途的挥发性药物经皮给药载体。
