Finally, our paper on the pharmacokinetic properties of LAT1 (L-type amino acid transporter 1)-utilizing prodrug of capsaicin was published in European Journal of Pharmaceutics and Biopharmaceutics. This was Janne's third and last article in his Ph.D. thesis and the aim was to achieve dual-targeting not only into the brain but also in the pancreas, and to have beneficial anti-inflammatory effects against the diseases interlinked in these organs, like neurodegenerative diseases and diabetes. Our prodrug had an extended exposure and improved target tissue distribution compared to the capsaicin, decreasing the peak concentrations in the brain and pancreas. The prodrug also showed promising effects against prostaglandin production after the LPS (lipopolysaccharide)-induction and was found safe in human blood in vitro assays. Moreover, since capsaicin alone suffers from poor bioavailability, quick metabolism, and(neuro)toxicity with high concentrations, which hinders its clinical use against a low-grade inflammation, the LAT1-utilizing prodrug approach can offer a great alternative to circumvent the unfavourable pharmaceutical issues related to highly potent natural compounds.
So Big Thanks to all co-authors for putting this together and congratulations for Janne, for finalizing and putting the period for the Ph.D. thesis! If you are interested, you can find more information about the publication from here: "Amino acid prodrug of capsaicin improves pharmacokinetic properties in the mouse brain and pancreas" (link).
