Oncotarget

Research Papers:

Bufalin-loaded bovine serum albumin nanoparticles demonstrated improved anti-tumor activity against hepatocellular carcinoma: preparation, characterization, pharmacokinetics and tissue distribution

Huiqing Zhang, Nian Huang, Geliang Yang, Qing Lin and Yonghua Su _

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Oncotarget. 2017; 8:63311-63323. https://doi.org/10.18632/oncotarget.18800

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Abstract

Huiqing Zhang1,*, Nian Huang1,*, Geliang Yang1, Qing Lin1 and Yonghua Su1

1Changhai Hospital of Traditional Chinese Medicine, Second Military Medical University, Shanghai 200433, China

*These authors have contributed equally to this work

Correspondence to:

Yonghua Su, email: [email protected]

Keywords: Bufalin, bovine serum albumin, nanoparticles, hepatocellular carcinoma

Received: November 08, 2016     Accepted: June 02, 2017     Published: June 28, 2017

ABSTRACT

Objective: To prepare and evaluate the liver-targeted drug delivery system of Bufalin with higher liver uptake and stronger antitumor activity against hepatocellular carcinoma.

Methods: Bufalin-loaded bovine serum albumin nanoparticle was prepared by desolvation method, to investigate the in vitro release performance and to evaluate the pharmacokinetic and tissue distribution. The antitumor activity against hepatocellular carcinoma was evaluated in vitro and in vivo, respectively.

Results: The Bufalin-loaded bovine serum albumin nanoparticle with an average particle size of 125.1 nm exhibited a sustained release behavior in vitro. The half-life, blood plasma area under the curve and apparent volume of distribution of Bufalin-loaded bovine serum albumin nanoparticle were significantly higher than that of Bufalin, whereas the clearance rate was lower than Bufalin group. The uptake of liver for Bufalin-loaded bovine serum albumin nanoparticle was 352.045 ± 35.665 ng/g while for Bufalin was 164.465 ± 48.080 ng/g (P < 0.01) at 5 min. The uptake of tumor for Bufalin-loaded bovine serum albumin nanoparticle was significantly higher than that of Bufalin both at 5 min (50.169 ± 11.708 ng/g, 93.415±13.828 ng/g, P < 0.01) and 15 min (43.683 ± 11.499 ng/g, 64.219 ± 17.684 ng/g, P > 0.05). Bufalin-loaded bovine serum albumin nanoparticle and Bufalin have similar antitumor activity in vitro. The tumor inhibition effect of Bufalin-loaded bovine serum albumin nanoparticle was stronger than that of Bufalin alone in vivo.

Conclusion: Bufalin-loaded bovine serum albumin nanoparticle is a promising liver-targeted drug delivery system with higher liver uptake and stronger antitumor activity against hepatocellular carcinoma.


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