Characteristics of sequential targeting of brain glioma for transferrin-modified cisplatin liposome.
Methods on how to improve the sequential targeting of glioma subsequent to passing of drug through the blood-brain barrier (BBB) have been occasionally reported. However, the characteristics involved are poorly understood. In the present study, cisplatin (Cis) liposome (lipo) was modified with transferrin (Tf) to investigate the characteristics of potential sequential targeting to glioma. In bEnd3/C6 co-culture BBB models, higher transport efficiency across the BBB and cytotoxicity in basal C6 cells induced by Cis-lipo(Tf) than Cis-lipo and Cis-solution, suggest its sequential targeting effect. Interestingly, similar liposomal morphology as that of donor compartment was first demonstrated in the receptor solution of BBB models. Meanwhile, a greater acquisition in the lysosome of bEnd3, distributed sequentially into the nucleus of C6 cells were found for the Cis-lipo(Tf). Pre-incubation of chlorpromazine and Tf inhibited this process, indicating that a clathrin-dependent endocytosis is involved in the transport of Cis-lipo(Tf) across the BBB.
Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, China; College of Pharmaceutical Science, Zhejiang Chinese Medical University, China.
Qing
Q
Lv
Li-Min
LM
Li
Min
M
Han
Xin-Jiang
XJ
Tang
Jin-Na
JN
Yao
Xiao-Ying
XY
Ying
Fan-Zhu
FZ
Li
Jian-Qing
JQ
Gao
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D001812:Blood-Brain Barrier / Q000378:metabolism; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002945:Cisplatin / Q000008:administration & dosage* / Q000737:chemistry; D005910:Glioma / Q000188:drug therapy* / Q000378:metabolism; D008081:Liposomes; D051379:Mice; D014168:Transferrin / Q000008:administration & dosage* / Q000737:chemistry
D000970:Antineoplastic Agents; D008081:Liposomes; D014168:Transferrin; D002945:Cisplatin