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

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Abstract

The aim of this study was to prepare a novel targeting nano drug delivery system of 2-methoxyestradiol (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 albumin nanoparticles (2-ME-BSANPs) were prepared by desolvation method, and then the activated folic acid was conjugated to 2-ME-BSANPs by covalent attachment (2-ME-FA-BSANPs). The size and zeta potential 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 apoptosis and affording higher antitumor efficacy against SMMC-7721 cells in vitro compared with 2-ME alone. Furthermore, the cell-cycle arrest of 2-ME-FA-BSANPs on the SMMC-7721 cells occurred at G2/M phase, and 2-ME-FA-BSANPs did not change the inhibition of the tumor mechanisms of 2-ME. Based on these results, it was concluded that albumin nanoparticles could be the promising nano carrier for 2-ME, and 2-ME-FA-BSANPs-targeting drug delivery system may be promising candidate for providing high treatment efficacy with minimal side effects in future cancer therapy.

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Acknowledgments

This work was supported by grants from the National Natural Science Foundation of China (No. 81273451).

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Authors and Affiliations

  1. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, People’s Republic of China

    Nan Zhang, Yadan Xia, Xiaojing Guo, Pei Wang, Shujuan Yan, Chunyun Lu, Danhua Cao & Zhenzhong Zhang

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  1. Nan Zhang
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  2. Yadan Xia
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  3. Xiaojing Guo
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  5. Shujuan Yan
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  8. Zhenzhong Zhang
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Correspondence to Zhenzhong Zhang.

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Zhang, N., Xia, Y., Guo, X. et al. Preparation, characterization, and in vitro targeted delivery of folate-conjugated 2-methoxyestradiol-loaded bovine serum albumin nanoparticles. J Nanopart Res 16, 2390 (2014). https://doi.org/10.1007/s11051-014-2390-6

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