TY  - JOUR
U1  - Wissenschaftlicher Artikel
A1  - Taiarol, Lorenzo
A1  - Bigogno, Chiara
A1  - Sesana, Silvia
A1  - Kravicz, Marcelo
A1  - Viale, Francesca
A1  - Pozzi, Eleonora
A1  - Monza, Laura
A1  - Carozzi, Valentina Alda
A1  - Meregalli, Cristina
A1  - Valtorta, Silvia
A1  - Moresco, Rosa Maria
A1  - Koch, Marcus
A1  - Barbugian, Federica
A1  - Russo, Laura
A1  - Dondio, Giulio
A1  - Steinkühler, Christian
A1  - Re, Francesca
T1  - Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics
JF  - Cancers
N2  - Glioblastoma is the most common malignant brain tumor with a high grade of recurrence, invasiveness, and aggressiveness. Currently, there are no curative treatments; therefore, the discovery of novel molecules with anti-tumor activity or suitable drug delivery systems are important research topics. The aim of the present study was to investigate the anti-tumor activity of Givinostat, a pan-HDAC inhibitor, and to design an appropriate liposomal formulation to improve its pharmacokinetics profile and brain delivery. The present work demonstrates that the incorporation of Givinostat in liposomes composed of cholesterol and sphingomyelin improves its in vivo half-life and increases the amount of drug reaching the brain in a mouse model. Furthermore, this formulation preserves the anti-tumor activity of glioblastoma in 2D and 3D in vitro models. These features make liposome-Givinostat formulations potential candidates for glioblastoma therapy.
KW  - glioblastoma
KW  - liposomes
KW  - HDCA inhibitor
KW  - brain
KW  - cancer
Y1  - 2022
UN  - https://nbn-resolving.org/urn:nbn:de:bsz:291:415-1618
U6  - https://doi.org/10.3390/cancers14122978
DO  - https://doi.org/10.3390/cancers14122978
VL  - 14
IS  - 12
SP  - 2978
ER  -