fondazione-don-carlo-gnocchi

COMING IN THE BRAIN: Liposomes for boosting drugs across the blood–brain barrier

  • Home
  • COMING IN THE BRAIN: Liposomes for boosting drugs across the blood–brain barrier

IT_Version

COMING IN THE BRAIN: Liposomes for boosting drugs across the blood–brain barrier

A study published by Cancers, a peer-reviewed, open access journal of oncology, demonstrates that the incorporation of an anti-cancer drug in liposomes strong improves its in vivo half-life and increases the amount of drug reaching the brain. These results were obtained thanks to the project IMMUN-HUB “Sviluppo di nuove molecole di seconda generazione per immunoterapia oncologica”, CUP E51B19000550007–Call HUB Ricerca e Innovazione, cofunded by POR FESR 2014–2020 (Regional Operational Programme, European Regional Development Fund).

The main topic of this work is glioblastoma, the most common malignant and lethal primary brain tumour that represents a challenging medical issue for neuro-oncologists. Herein, it was shown that the nanoformulation of Givinostat, a pan-HDAC inhibitor, in liposomes promotes a 2.5-fold increase in the drug half-life in the bloodstream and a 6-fold increase in the amount of drug entering the brain in healthy mice, without any signs of overt toxicity. Moreover, using 2D and 3D in vitro models, they showed that liposomes-Givinostat counteracts tumour cell growth by modulating different biochemical processes. As there are currently no curative treatments for glioblastoma, the availability of appropriated drug delivery systems is an important research topic. Moreover, given the easy production, scale up and ductility of liposomes, this approach may provide opportunities to build up clinically compliant nano-objects to address the complexity of several brain disorders.

newsletter luglio

150-nm-sized liposomes inhibited human GBM cell growth in 2Dand 3D models by inducing a time- and dose-dependent reduction in cell viability, reduction in the receptors involved in cholesterol metabolism, and reduction in HDAC activity. In addition, liposome-Givinostat showed a 2.5-fold increase in the drug half-life in the bloodstream and a 6-fold increase in the amount of drug entering the brain in healthy mice.
[Taiarol L, Bigogno C, Sesana S, Kravicz M, Viale F, Pozzi E, Monza L, Carozzi VA, Meregalli C, Valtorta S, Moresco RM, Koch M, Barbugian F, Russo L, Dondio G, Steinkühler C, Re F. Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics. Cancers (Basel). 2022 Jun 16;14(12):2978. doi: 10.3390/cancers14122978].

 These promising results were obtained thanks to the close cooperation between different institutions and SMEs, leaded by Prof. Francesca Re from CNLAB of University Milano-Bicocca (www.cnlab.medicina@unimib.it).