a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , P.R. China.
b Faculty of Chemical Engineering , Kunming University of Science and Technology , Kunming , P.R. China.
Pharm Dev Technol. 2017 Aug;22(5):669-677. doi: 10.1080/10837450.2016.1221429. Epub 2016 Aug 30.
We report the preparation of inclusion complexes between rhein and four polyamine-modified β-cyclodextrins, namely amino-β-cyclodextrins (NH-βCD), ethylenediamine-β-cyclodextrins (EN-βCD), diethylenetriamine-β-cyclodextrins (DETA-βCD) and triethylenetetramine-β-cyclodextrins (TETA-βCD) using suspension method. The solution and solid state forms of the inclusion complexes of rhein with polyamine-β-cyclodextrins were characterized by multiple techniques. Additionally, saturated solution and MTT methods were implemented to assess the water solubilization and in vitro cytotoxicity of the inclusion complexes, respectively. The results suggested that rhein was encapsulated within the CD cavity to form a 1:1 host-guest inclusion complex. Notably, a significant enhancement of the water solubility and in vitro cytotoxicity of rhein was found in the form of inclusion complex with polyamine-β-cyclodextrin.
我们报告了利用悬浮法制备大黄酸与四种聚胺修饰的β-环糊精（即氨基-β-环糊精（NH-βCD）、乙二胺-β-环糊精（EN-βCD）、二乙烯三胺-β-环糊精（DETA-βCD）和三乙烯四胺-β-环糊精（TETA-βCD））的包合物。通过多种技术对大黄酸与聚胺-β-环糊精的包合物的溶液和固态形式进行了表征。此外，还采用饱和溶液法和 MTT 法分别评估了包合物的增溶作用和体外细胞毒性。结果表明，大黄酸被包封在 CD 空腔内形成 1:1 的主客体包合物。值得注意的是，大黄酸与聚胺-β-环糊精形成包合物形式时，其水溶性和体外细胞毒性显著增强。
