Development of a potential nano-based delivery system combining Colchicine-loaded lipid nanocapsules and BIOT-NFL-peptide to target glioblastoma

Peptide conjugated-nanodrug is one of the most studied new treatment options in the field of cancer, including glioblastoma (GBM). This tumour, GBM, is a difficult to treat brain tumour mainly due to its location and the complexity of targeting tumour cells. A promising GBM-targeting peptide (NFL-TBS.40-63) is a cell penetrating peptide (CPP) that has previously demonstrated selectivity against GBM cells and also a capacity to damage their microtubule network at appropriate concentrations. Here, a potential nano-based delivery system was developed by coupling the biotinylated-NFL-peptide (BIOT-NFL) with lipid nanocapsules (LNCs) loaded with Colchicine (Col), an anti-microtubule agent with potent anticancer activity. The effect of BIOT-NFL and free Colchicine was first evaluated on GBM cells. Colchicine was then loaded in lipid nanocapsules (Col-loaded LNCs) and the obtained nanocapsules were characterized for particle size, morphology, encapsulation efficiency and <i>in vitro</i> release, and then coupled with the BIOT-NFL-peptide. Interestingly, a potential nanosystem composed of peptide-nanofibers (formed from BIOT-NFL) decorated with Col-LNCs was observed by electron microscopic examination. Finally, the effects of this BIOT-NFL coupled to Col-LNCs were evaluated <i>in vitro</i> on GBM cells. This new nanosystem may offer a promising strategy for GBM targeted therapy.