Angiopep-2 and transferrin co-modified liposome for targeted drug delivery across the blood-brain barrier / 第二军医大学学报

ABSTRACT

Objective To prepare angiopep-2 and transferrin co-modified liposomes (ANG/TF-LPs) and to observe their propertyof passing the blood-brain barrier (BBB). Methods ANG/TF-LPs were prepared by film-ultrasonic method. The particle size, Zeta potential and stability in fetal bovine serum (FBS) of ANG/TF-LPs were evaluated. The cellular uptake of ANG/TF-LPs by bEnd. 3 cells in vitro was observed to evaluate the targeting efficiency. The in vitro BBB model was used to evaluate the ability of liposomes passing the BBB. Results The diameter of the prepared ANG/TF-LPs was (93.2 ± 13.5) nm, the Zeta potential was (7.55 ± 1.85) mV, and they were stable in FBS within 24 h. tt was found that the uptake of ANG/TF-LPs by bEnd. 3 cells was 2.9, 2.4 and 4.8 folds those of transferrin modified liposomes (TF-LPs), angiopep-2 modified liposomes (ANG-LPs) and liposomes (LPs), respectively (P < 0.01). The efficiency of ANG/TF-LPs passing the BBB was 3.1, 2.9 and 5.4 folds those of TF-LPs, ANG-LPs and LPs, respectively (P < 0.01). Conclusion The angiopep-2 and transferrin co-modified liposomes are easy to prepare, and the modification can enhance the BBB passing ability, making the prepared liposomes a promising brain drug delivery system.