Parkinson’s disease (PD) is the second most common neurodegenerative disease, which accompanied with striatal dopamine (DA) deficiency and neuronal loss in the substantia nigra. Current strategies for PD are challenged by the presence of the blood-brain barrier (BBB) that significantly limits the effective drug concentration in a patient’s brain for therapeutic response throughout various stages of PD. Resveratrol (RES) holds the potential for α-synuclein clearance to treat PD. However, its applications are limited due to its low bioavailability and poor permeability through BBB in a free form. To overcome the above problems associated with the delivery of RES across the BBB for improved PD treatment, we herein designed RES-loaded lactoferrin (Lf)-conjugated PEGylated nanoscale graphene oxide (GO) (Lf-PEG-GO-RES). In this system, GO serves as a molecular carrier due to its excellent drug loading capacity, ultrahigh surface area and easy surface functionalization. The surface modification with Lf is used to assist the RES across the BBB by transcytosis through vascular endothelial cells. This multifunctional Lf-PEG-GO-RES formulation could be an effective, safe and amenable choice with higher therapeutic relevance and fewer unwanted complications than conventional delivery systems for PD treatment in the near future.