The formation of inclusion complexes with cyclodextrin and derived materials is one of its main applications, and is also of great interest to industry. Classic solubilization and solvent removal processes require a long time and a loss of the compound of interest, which usually remains in a phase different from that of the complex.
In this study we have determined the complexation of progesterone, a lipophilic hormone used in hormone replacement therapy, with cyclodextrins (CD) and cyclodextrin-based nanosponges (CD-NS), applying the kneading process assisted by a ball-milling, obtaining :
- Encapsulation Efficiency: Various molar ratios of β-CD and progesterone were evaluated, finding that even with a 1:1 ratio, all the drug was efficiently encapsulated. Analyses using FTIR, TGA, and DSC confirmed this complete encapsulation.
- Release Profile: Dialysis studies showed that the obtained complexes had a faster and more gradual release profile compared to the free drug, with slight differences between the formulations. This suggests controlled and sustained release of progesterone from the complexes.
- Effectiveness in MCF-7 Cells: The action of the complexes against the MCF-7 breast cancer cell line demonstrated an influence of proper complexation on their effectiveness, showing improved cytotoxicity compared to the physical mixture of progesterone and CD, without removing the extra-drug from the formulation.
The ball-milling kneading technique emerges as a promising method for complex formation, offering quick, efficient, and economical encapsulation. These findings can lead to significant advancements in the formulation of hormone therapies and controlled drug delivery.
Reference:
Matencio, A., Bisericaru, D. M., Conesa, I., Er-Rahmani, S., Pedrazzo, A. R., López-Nicolás, J. M., & Trotta, F. (2024). STUDY OF PROGESTERONE COMPLEXATION IN CYCLODEXTRINS AND CYCLODEXTRIN-BASED NANOSPONGES AS AN EXAMPLE OF SOLVENT-FREE COMPLEXATION. Journal of Drug Delivery Science and Technology, 105893. https://doi.org/10.1016/j.jddst.2024.105893