Zong Shiyu, Pu Yiqiong, Li Suyun, Xu Benliang, Zhang Yong, Zhang Tong, Wang Bing
a Experimental Center for Teaching and Learning , Shanghai University of Traditional Chinese Medicine , Shanghai , China.
b School of Pharmacy , Shanghai University of Traditional Chinese Medicine , Shanghai , China.
Artif Cells Nanomed Biotechnol. 2018;46(sup1):324-335. doi: 10.1080/21691401.2017.1423497. Epub 2018 Jan 9.
Paeonol, as the main phenolic compound isolated from the Chinese herbs, has been confirmed to present anti-inflammatory effects on ulcerative colitis (UC) in our previous study. However, its poor solubility has hindered its development of being a favourable pharmaceutical product in treating colon diseases. In this study, we prepared the colon-specific delivery system (Pae-SME-CSC) with paeonol-loaded self-microemulsion (Pae-SMEDDS), and evaluated its in vitro and in vivo properties, especially the anti-inflammatory effects on UC rats. The anti-inflammatory effects were evaluated by the disease activity index, colon weight/length ratio, and macroscopic damage and microscopic damage scores. IL-17, IL-6, and TGF-β1 levels were also determined by enzyme-linked immunosorbent assay. The results showed that Pae-SME-CSC had good colon-targeting property in vivo and in vitro, with favourable stability. Efficacy evaluation showed that the dose of the paeonol group (100 mg/kg) exhibited no significant effect on UC (p > .05, compared with the model group), while the Pae-SME-CSC group (100 mg/kg) showed better anti-UC effects (p < .01 or p < .05), and its anti-inflammatory effect was close to that of the paeonol group (200 mg/kg) (p > .05). These results indicated that the developed Pae-SME-CSC was suitable for colon-specific drug delivery.
丹皮酚作为从中药中分离出的主要酚类化合物，在我们之前的研究中已被证实对溃疡性结肠炎（UC）具有抗炎作用。然而，其溶解度差阻碍了它成为治疗结肠疾病的理想药物。在本研究中，我们制备了载有丹皮酚的自微乳（Pae-SMEDDS）结肠特异性递送系统（Pae-SME-CSC），并评估了其体外和体内性质，特别是对UC大鼠的抗炎作用。通过疾病活动指数、结肠重量/长度比以及宏观损伤和微观损伤评分来评估抗炎作用。还通过酶联免疫吸附测定法测定白细胞介素-17（IL-17）、白细胞介素-6（IL-6）和转化生长因子-β1（TGF-β1）的水平。结果表明，Pae-SME-CSC在体内和体外均具有良好的结肠靶向性，稳定性良好。疗效评估表明，丹皮酚组（100mg/kg）对UC无显著影响（与模型组相比，p＞0.05），而Pae-SME-CSC组（100mg/kg）显示出更好的抗UC效果（p＜0.01或p＜0.05），其抗炎作用接近丹皮酚组（200mg/kg）（p＞0.05）。这些结果表明，所研制的Pae-SME-CSC适用于结肠特异性药物递送。
