Antioxidant based Solid Lipid Nanoparticles: in vitro studies on the administration of citicoline for supporting anti-Parkinson therapy

INTRODUCTION: Parkinson disease (PD) is intensively investigated not only due to its neurotransmission abnormalities but also for the increasingly recognized involvement of mitochondrial disfunctions, Here, in order to face both issues, Dopamine-Gelucire® 50/13 based solid lipid nanoparticles (SLNs) administering the antioxidant citicoline (CIT) were formulated by us and were studied in vitro for application in PD treatment (1,2). EXPERIMENTAL: To develop such SLNs for nasal administration, SLNs were prepared following the melt homogenization method and their physicochemical features were investigated together with TEM Microscopy, X-rays diffraction and in vitro cell viability studies. RESULTS: SLNs showed a mean diameter of 201 nm, −2.20 mV as zeta potential and a high percentage of entrapped CIT. Biological evaluation showed that pre‐treatment of SH‐SY5Y dopaminergic cells with CIT‐SLNs (50 μM) before the addition of 40 μM 6‐hydroxydopamine (6‐OHDA) to mimic Parkinson’s disease’s degenerative pathways counteracts the cytotoxic effects induced by the neurotoxin, increasing cell viability and maintaining both nuclear and cell morphology. DISCUSSION: Biological data suggest an enhanced protection exerted by CIT‐SLNs with respect to free CIT and indicate that, despite its polar characteristics, CIT is encapsulated at high levels in our lipophilic SLN carriers, disclosing a potential use of CIT‐SLNs as a novel nose-to-brain delivery strategy for PD applications.