Metal-organic frameworks (MOFs) consisting of γ-cyclodextrin and potassium were used to incorporate folic acid clusters. The molar ratio of folic acid to CD reached 2:1 in this formulation. This “Ship-in-Bottle” strategy has led to a 1450 fold increase of the apparent solubility of folic acid. The bioavailability in rats was enhanced by a factor of 1.48 as compared to free folic acid.
Concerning the mechanism it was assumed that either folic acid nanoclusters were formed inside the hydrophilic cavities and/or folic acid was included inside dual CD units in CD-MOF. This dual incorporation mechanism is a novel approach to increase the drug apparent solubility and bioavailability, and could be a promising strategy for other poorly soluble drugs.
Folic acid (left) and model of γ-cyclodextrin/potassium nano MOF (https://pubs.acs.org/cen/news/88/i35/8835notw4.html)
Xu, J., Wu, L.. Guo, T., Zhang, G., Wang, C., Li, H., Li, X., Singh, V., Chen, W., Gref, R., Zhang, J. A “Ship-in-a-Bottle” strategy to create folic acid nanoclusters inside the nanocages of γ-cyclodextrin metal-organic frameworks. Int. J. Pharm, 2018 (in press) https://doi.org/10.1016/j.ijpharm.2018.11.074