Transferrin-functionalized liposomes loaded with vitamin VB12 for Alzheimer?s disease therapy

Despite the efforts of the pharmaceutical and research sectors, Alzheimer's disease (AD) remains incurable, imposing the demand for new effective strategies. Vitamin B12 (VB12) has aroused interest due to its in vitro anti-amyloidogenic properties. However, the high molecular weight and hydrophilicity of VB12 are the main ob-stacles to its clinical application by hindering its passage through the blood-brain barrier (BBB). In recent years, drug delivery systems (DDSs) capable of transporting molecules across the BBB have gained attention for their effective brain delivery. In this work, VB12-loaded liposomes functionalized with transferrin (Tf) were produced, envisaging the dual-targeting of VB12 to the BBB and neuronal cells, due to the overexpression of Tf receptors in these cells. The produced liposomes presented sizes smaller than 200 nm, with low polydispersity and neutral zeta potential, being suitable for brain delivery. The nanoparticles exhibited an adequate encapsulation effi-ciency, a sustained release of VB12 for 9 days, and physical stability at storage conditions for up to 2 months. The developed nanosystem was capable of delaying the formation of A beta fibrils and disrupting mature fibrils, high-lighting its great potential for the prevention and treatment of AD.

Automated summary

This study developed a VB12-loaded liposome nanosystem capable of dual-targeting VB12 to the blood-brain barrier (BBB) and neuronal cells, delaying the formation of Aβ fibrils and disrupting mature fibrils. This research has significant potential for the prevention and treatment of AD.