Melatonin/HP beta CD complex: Microwave synthesis, integration with chitosan scaffolds and inhibitory effects on MG-63CELLS

作者：Topal Bedriye; Altindal Damla Cetin; Gumusderelioglu Menemse^*

来源：International Journal of Pharmaceutics, 2015, 496(2): 801-811.

DOI：10.1016/j.ijpharm.2015.11.028

• 2-Hydroxypropyl-beta-cyclodextrin
• Melatonin
• Microwave
• Inclusion complex

In this study, melatonin/2-hydroxypropyl-beta-cyclodextrin (HP beta CD) 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 HP beta CD 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, H-1 NMR and C-13 NMR studies. Both of pure melatonin and melatonin/HP beta CD 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 9 mM 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/HP beta CD inclusion complex loaded chitosan scaffolds could be considered as an alternative system for the human osteosarcoma therapy.

• 出版日期2015-12-30