通过机械化学法制备姜黄素自微乳固体分散体以提高生物利用度和细胞毒性活性。
Preparation of curcumin self-micelle solid dispersion with enhanced bioavailability and cytotoxic activity by mechanochemistry.
机构信息
a National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology , Hangzhou , PR China.
b Institute of Chemical Kinetics and Combustion , Novosibirsk , Russia.
出版信息
Drug Deliv. 2018 Nov;25(1):198-209. doi: 10.1080/10717544.2017.1422298.
An amorphous solid dispersion (SD) of curcumin (Cur) with disodium glycyrrhizin (NaGA) was prepared by mechanical ball milling. Curcumin loaded micelles were self-formed by NaGA when SD dissolved in water. The physical properties of Cur SD in solid state were characterized by differential scanning calorimetry, X-ray diffraction studies, and scanning electron microscope. The characteristics of the sample solutions were analyzed by reverse phase HPLC, UV-visible spectroscopy, H NMR spectroscopy, gel permeation LC, and transmission electron microscopy. In vitro cytotoxic tests demonstrated that Cur SD induced higher cytotoxicity against glioblastoma U-87 MG cells than free Cur. Besides, an improvement of membrane permeability of Cur SD was confirmed by parallel artificial membrane permeability assay. Further pharmacokinetic study of this SD formulation in rat showed a significant ∼19-fold increase of bioavailability as comparing to free Cur. Thus, Cur SD provide a more potent and efficacious formulation for Cur oral delivery.
通过机械球磨法制备了姜黄素（Cur）与甘草酸钠（NaGA）的无定形固体分散体（SD）。当 SD 在水中溶解时，NaGA 自形成载姜黄素胶束。通过差示扫描量热法、X 射线衍射研究和扫描电子显微镜对 Cur SD 在固态下的物理性质进行了表征。通过反相高效液相色谱法、紫外可见分光光度法、H NMR 光谱法、凝胶渗透 LC 和透射电子显微镜分析了样品溶液的特性。体外细胞毒性试验表明，与游离姜黄素相比，Cur SD 对神经胶质瘤 U-87MG 细胞的细胞毒性更高。此外，通过平行人工膜渗透试验证实了 Cur SD 透膜能力的提高。该 SD 制剂在大鼠中的药代动力学研究表明，与游离姜黄素相比，生物利用度显著提高了约 19 倍。因此，Cur SD 为姜黄素的口服递送提供了一种更有效、更有效的制剂。
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