期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 579, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119134
关键词
5-Demethyltangeretin (5-DTAN); Self-microemulsifying delivery system (SMEDS); Colon cancer
资金
- Ministry of Science and Technology [108-2321-B-002-020, 108-2320-B-002-016-MY3]
5-Demethyltangeretin (5-DTAN), a polymethoxylated flavone found in citrus peels, exhibits highly potent anti-cancer activity. However, 5-DTAN is a hydrophobic compound with poor aqueous solubility, which limits its oral bioavailability and efficacy. In this study, we aimed to develop and characterize an optimal self-microemulsifying delivery system (SMEDS) formulated for 5-DTAN and to assess its anticancer activity in a xenograft model. SMEDS is a lipid-based formulation and typically comprises oil, surfactant, and co-surfactant. The results from our solubility and compatibility test revealed that ethyl oleate and d-limonene were appropriate for use as an oil phases. The optimal formulation comprised ethyl oleate/d-limonene (10%/5%), Cremophor (R) EL (59.5%), and PEG 400 (25.5%). With this optimal formulation, the mean particle size was 97.1 +/- 6.50 nm with the highest 5-DTAN loading (3.01 +/- 0.38 mg/mL) determined by photon correlation spectroscopy. The transmission electron microscopy (TEM) morphology of 5-DTAN microemulsion droplets demonstrated a spherical shape and uniform size. Our findings suggest that using 5-DTAN loading SMEDS is an effective approach for inhibiting tumor growth in colon cancer xenograft mice. In summary, this study is the first to successfully demonstrate that oral administration of 5-DTAN-loaded SMEDS serves as a promising nutraceutical for cancer prevention.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据