Fabrication and evaluation a transferrin receptor targeting nano-drug carrier for cerebral infarction treatment

After cerebral infarction, the regeneration of microvascular played an important role in the recovery. Ginsenoside Rg1 (Rg1) had good effects on promoting angiogenesis and neuro-protection in cerebral infarction treatment. However, the blood-brain barrier (BBB) restricted Rg1 to enter into cerebral tissue. Transferrin receptor (TfR) was over-expressed in the BBB. In this study, we fabricated a TfR targeting nano-carrier (PATRC) to penetrate the BBB for treatment of cerebral infarction. A TfR targeted peptide was conjugated with the nano-carrier wrapped hydrophobic Rg1. The nanoscale size (132 +/- 12 nm), polydispersity index (PDI =0.29) and the zeta potential (-38mv) were tested with dynamic light scattering optical system. Surface morphology (ellipse, mean diameter 122 +/- 26 nm) was detected by transmission electron microscope (TEM). PATRC implement cell targeting ability on rat brain microvascular endothelial cells RBE4 in vitro detected by immunofluorescence and flow cytometry methods. Comparing with Rg1 threated group, the PATRC exhibited more prominent ability on the tube formation ability (p<.05) in vitro. Comparing with the Rg1 treated group, PATRC penetrated BBB in vivo detected by HPLC, decreased the brain infarction volume tested with TTC staining and promoted regeneration of microvascular in infarction zone detected by CD31 immunofluorescence. PATRC has great potentiality for wide application in clinic.