Yao ZhongWei, Zhang Wei, Hu Yehong, An Zhentao, Fang Zhijun, Wang Jing, Zhang Zhenhai
Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, 100 Shizi Road, Nanjing, Jiangsu, 210028, China.
State Key Laboratory of Oral Drug Delivery Systems of Chinese Materia Medica, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, Jiangsu, 210028, China.
Drug Deliv Transl Res. 2025 Apr;15(4):1235-1248. doi: 10.1007/s13346-024-01666-y. Epub 2024 Jul 7.
Eugenol possesses anti-inflammatory and antioxidant properties, and may serve as a potential therapeutic agent for hepatic fibrosis. However, the development of solid eugenol formulations is challenging due to its volatility. To address this issue, this study employed porous silica to adsorb solidified eugenol. The solidified powder was characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). In addition, the differences in in vitro release and oral bioavailability between eugenol and solidified eugenol powder were investigated. The effectiveness of eugenol and eugenol powder in treating liver fibrosis was investigated using enzyme-linked immunosorbent assay (ELISA), polymerase chain reaction (PCR), and histopathological observations. Our results indicate that porous silica can effectively solidify eugenol into powder at a lower dosage. Furthermore, we observed that porous silica accelerates eugenol release in vitro and in vivo. The pharmacodynamic results indicated that eugenol has a positive therapeutic effect against hepatic fibrosis and that porous silica does not affect its efficacy. In conclusion, porous silica was able to solidify eugenol, which may facilitate the preparation and storage of solid formulations.
丁香酚具有抗炎和抗氧化特性，可能成为肝纤维化的潜在治疗药物。然而，由于丁香酚的挥发性，开发其固体剂型具有挑战性。为解决这一问题，本研究采用多孔二氧化硅吸附固化丁香酚。利用傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和扫描电子显微镜（SEM）对固化粉末进行了表征。此外，还研究了丁香酚与固化丁香酚粉末在体外释放和口服生物利用度方面的差异。采用酶联免疫吸附测定（ELISA）、聚合酶链反应（PCR）和组织病理学观察研究了丁香酚和丁香酚粉末治疗肝纤维化的有效性。我们的结果表明，多孔二氧化硅能够以较低剂量有效地将丁香酚固化成粉末。此外，我们观察到多孔二氧化硅在体外和体内均可加速丁香酚的释放。药效学结果表明，丁香酚对肝纤维化具有积极的治疗作用，且多孔二氧化硅不影响其疗效。总之，多孔二氧化硅能够固化丁香酚，这可能有助于固体剂型的制备和储存。
