Solvent-free cyclodextrin nanosponges complexes for increasing the bioavailability

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Recently the Francesco Trotta’s group of the University of Turin (Italy) has finalized and published the preliminar results that he introduced in ICS20 (Messina). The research was focused on two importact aspects:

  1. To effectivelly complex a drug, in this case the nutraceutical Kynurenic acid (KYNA) in HPβ-CD and βNS-CDI (carbonate βCD-NS using the ball-milling solvent free approach
  2. To study the increase of bioavailabilty and biochemical profile in vivo.

The use of kneading permited to overcome all the limitations related to poorly soluble or insoluble compoundsas KYNA, permitting to avoid the use of solvents completely and speed-up the preparation of the inclusion complex. The “classic” solvent approach usually uses 3 days (1 day of mixing, 2 days of lyophilization) but the ball milling only takes 30 min of complex preparation, considerably reducing the time to get ready to use complexes, at the end these complexes presented similar FTIR and TGA profiles.

Secondly, a higher bioavailability with βNS-CDI in comparison to HPβ-CD and the control was found, respectively. Different parameters, such as the Cmax or clearance, were improved when the bioactive compound was complexed. Several biological parameters were also improved and the complex formulation of KYNA reduced the temporal oxidative stress damage in the kidney and liver

As conclusion, we can say that these results suggest an important future application of CD-NSs for the oral administration of drugs, supplementation of nutraceuticals, and its stabilization.

[1] Monfared, Y. K., Pedrazzo, A. R., Mahmoudian, M., Caldera, F., Zakeri-Milani, P., Valizadeh, H., … & Trotta, F. (2022). Oral Supplementation Of Solvent-Free Kynurenic Acid/Cyclodextrin Nanosponges Complexes Increased Its Bioavailability. Colloids and Surfaces B: Biointerfaces, 113101. DOI: 10.1016/j.colsurfb.2022.113101

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