文献类型：期刊文献

英文题名：Dual-modified bufalin loaded liposomes for enhanced tumor targeting

作者：Zhang, Yongchao[1,2];Tian, Zhenfen[1,2];Zhao, Xiaotong[1,2];Li, Na[3,4];Garamus, Vasil M.[5];Yin, Peihao[6];Zou, Aihua[1,2]

机构：[1]East China Univ Sci & Technol, Sch Chem & Mol Engn, State Key Lab Bioreactor Engn, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Inst Appl Chem, Shanghai 200237, Peoples R China;[3]Natl Ctr Prot Sci Shanghai, Shanghai 200237, Peoples R China;[4]Shanghai Inst Biochem & Cell Biol, Shanghai 200237, Peoples R China;[5]Helmholtz Zentrum Geesthacht, Ctr Mat & Coastal Res, D-21502 Geesthacht, Germany;[6]Shanghai Univ Tradit Chinese Med, Putuo Hosp, Dept Gen Surg, Shanghai 200062, Peoples R China

年份：2019

卷号：571

起止页码：72

外文期刊名：COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS

收录：;EI(收录号：20191306699774);WOS:【SCI-EXPANDED(收录号:WOS:000466612200010)】；

基金：We gratefully acknowledge the support of this work by the National Natural Science Foundation of China (Grant No. 21573070), the National Natural Science Foundation of China (Grant No. 21872051). We thank the staff of the BL19U2 beamline at the National Center for Protein Science Shanghai and the Shanghai Synchrotron Radiation Facility for assistance during data collection.

语种：英文

外文关键词：RGD peptide; Liposome; Bufalin; PEG; Active targeted ligand

摘要：Bufalin, a traditional oriental medicine, has been incorporated into liposomes for better targeted drug delivery. Bufalin-loaded liposome (L-BF), bufalin-loaded PEGylated liposome (L-PEG-BF) and bufalin-loaded RGD targeted PEGylated liposome (L-RGD-PEG-BF) were successfully developed with homogeneous particle size and sufficient physical stability in 30 days. The entrapment efficiency (EE) and drug loading efficiency (DL) of bufalin in these liposomes were about 85.4-90.6% and 6.0-6.6%, respectively. The morphologies of these liposomes were determined as uniquely recognizable phospholipid bilayers of the vesicle membrane by the measurements of transmission electron microscopy (TEM) and small angle X-ray scattering (SAXS). L-BF, L-PEG-BF and L-RGD-PEG-BF exhibited improved anticancer efficacy compared to free bufalin. Moreover, L-RGD-PEG-BF showed higher inhibition on the proliferation of A549 cells than the other two non-targeted bufalin liposomes in cytotoxicity study, and the growth inhibition concentration (IC50) of L-RGD-PEG-BF (8.62 +/- 0.74 ng/mL) was much lower than pure bufalin (20.37 +/- 2.31 ng/mL). Both confocal and apoptosis assay indicated that L-RGD-PEG-BF was easier to be taken into cancer cells than non-targeted bufalin liposomes. Therefore, L-RGD-PEG-BF is expected to be an effective drug carrier for bufalin delivery in tumor treatment.