Preparation, characterization, and in vitro targeted delivery of folate-conjugated 2-methoxyestradiol-loaded bovine serum albumin nanoparticles

【作者】 Nan Zhang • Yadan Xia • Xiaojing Guo •Pei Wang • Shujuan Yan • Chunyun Lu •Danhua Cao • Zhenzhong Zhang，

【期刊名】 Journal of Nanoparticle Research

【影响因子】 2014年: 2.87

【作者单位】 School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China

【年，卷(期)：页码】2014, 16: 2390

【关键词】 2-Methoxyestradiol Bovine serum albumin Folic acid Targeting delivery system Nanomedicine

【摘要】The aim of this study was to prepare a novel targeting nano drug delivery system of 2-meth-oxyestradiol (2-ME) based on the folic acid-modified bovine serum albumin, in order to improve the clinical application disadvantages and antitumor effect of 2-ME. In this study, 2-methoxyestradiol-loaded albu-min nanoparticles (2-ME-BSANPs) were prepared by desolvation method, and then the activated folic acid was conjugated to 2-ME-BSANPs by covalent attach-ment (2-ME-FA-BSANPs). The size and zeta poten-tial of 2-ME-FA-BSANPs were about 208.8 ± 5.1 nm and -32.70 ± 1.01 mV, respectively. 2-ME loading efficiency and loading amount of the nanoparticles were 80.49 ± 3.80 and 10.25 ± 1.59 %, respectively. SEM images indicated that 2-ME-FA-BSANPs were of a round shape, similar uniform size, and smooth surface. Studies on drug release indicated that 2-ME-FA-BSANPs had the properties of sustained and controlled release, which provided them with the ability to fight continually against cancer cells. Internalization analysis demonstrated that 2-ME-FA-BSANPs-targeting drug delivery system could get efficiently transferred into the cells through the folic acid-mediated endocytosis, leading to higher

【全文链接】https://link.springer.com/article/10.1007/s11051-014-2390-6