Poly-ion complex micelles effectively deliver CoA-conjugated CPT1A inhibitors to modulate lipid metabolism in brain cells
West Kristian D. Paraiso, Jesús García-Chica, Xavier Ariza, Sebastián Zagmutt, Shigeto Fukushima, Jordi García, Yuki Mochida, Dolors Serra, Laura Herrero, Hiroaki Kinoh, Núria Casals, Kazunori Kataoka, Rosalía Rodríguez‐Rodríguez, Sabina Quader
Abstract
by 2 to 4-fold over the free drug-treated U87MG after long-term incubation. To measure the cellular uptake of these CoA-adduct loaded PIC micelles, we synthesized a fluorescent CoA derivative and prepared Fluor-CoA micelles which showed efficient internalization in the cell lines, both in 2D and 3D culture models, especially in neurons where uptake reached up to 3-fold over the free dye. Our results starkly demonstrate that the PIC micelles are a promising delivery platform for anionic inhibitors of CPT1A in glioma cells and neurons, laying the groundwork for future research or clinical applications.