Hacettepe University, Chemical Engineering Department, 06800 Beytepe, Ankara, Turkey.
Hacettepe University, Chemical Engineering Department, 06800 Beytepe, Ankara, Turkey.
Int J Pharm. 2015 Dec 30;496(2):801-11. doi: 10.1016/j.ijpharm.2015.11.028. Epub 2015 Nov 19.
In this study, melatonin/2-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complex was prepared by using microwave irradiation in a very short time. Phase-solubility studies indicated a linear increase in the solubility of melatonin with HPβCD demonstrating Higuchi's AL-type phase solubility profiles and the formation of 1:1 stoichiometric inclusion complexes. Also, the ability of inclusion complex formation was promoted at microwave conditions compared to room conditions. The structure of inclusion complex was determined by FTIR, DSC, XRD, (1)H NMR and (13)C NMR studies. Both of pure melatonin and melatonin/HPβCD inclusion complex were loaded into the chitosan scaffolds that were prepared by freeze-drying method and the effect of released melatonin on human osteosarcoma cells (MG-63) was investigated in vitro. Approximately 9mM melatonin concentration caused time dependent cell death by reducing the proportion of the cells in the G2/M phase rather than S phase. In conclusion, melatonin/HPβCD inclusion complex loaded chitosan scaffolds could be considered as an alternative system for the human osteosarcoma therapy.
在这项研究中，通过在极短的时间内使用微波辐射制备了褪黑素/2-羟丙基-β-环糊精（HPβCD）包合物。相溶解度研究表明，褪黑素的溶解度随 HPβCD 的线性增加，表明 Higuchi 的 AL 型相溶解度曲线和 1:1 化学计量比的包合物的形成。此外，与室温条件相比，在微波条件下促进了包合物形成的能力。通过 FTIR、DSC、XRD、（1）H NMR 和（13）C NMR 研究确定了包合物的结构。将纯褪黑素和褪黑素/HPβCD 包合物都负载到壳聚糖支架中，壳聚糖支架是通过冷冻干燥法制备的，并在体外研究了释放的褪黑素对人骨肉瘤细胞（MG-63）的影响。约 9mM 的褪黑素浓度通过降低 G2/M 期而不是 S 期细胞的比例导致时间依赖性细胞死亡。总之，负载褪黑素/HPβCD 包合物的壳聚糖支架可被视为人类骨肉瘤治疗的替代系统。
