Improved Oral Bioavailability and Liver Targeting of Sorafenib Solid Lipid Nanoparticles in Rats

被引:0
|
作者
Haipeng Wang
Huiyun Wang
Wenlong Yang
Mengjie Yu
Shuilin Sun
Baogang Xie
机构
[1] Nanchang University,Department of Infectious Diseases, The Second Affiliated Hospital of Nanchang University, School of Pharmaceutical Science
来源
AAPS PharmSciTech | 2018年 / 19卷
关键词
sorafenib; solid lipid nanoparticle; evaluation; liver targeting; pharmacokinetics;
D O I
暂无
中图分类号
学科分类号
摘要
Minimal information is available on the oral bioavailability and liver-targeting properties of sorafenib solid lipid nanoparticles (SRF-SLNs) in rats. In this study, SRF-SLNs were prepared via the combined methods of high-speed shearing and ultrasonic treatment. SRF-SLN formulations were also optimized. Particle size, zeta potential, entrapment efficiency (EE), and drug loading (DL) were used as indices for the evaluation of the as-prepared SRF-SLNs. SRF concentration was determined by the high-performance liquid chromatography method. Results showed that the average EE and DL of SRF-SLNs were 89.87 and 5.39%. The average particle size, polydispersity index, and zeta potential of SRF-SLNs were 77.16 nm, 0.28, and − 18.1 mV, respectively. The results of the stability test showed that SRF-SLNs remained stable for more than 1 month at room temperature. After oral administration to rats (7.5 mg/kg), the liver-targeting evaluation results showed that the average drug selectivity index value of SRF-SLNs was 2.20 times higher, than that of the SRF-suspension. Furthermore, the area under the concentration–time curve of SRF increased by 66.7% in the SRF-SLN group comparing with that in the SRF-suspension. Our results suggested that SLNs were a promising approach for the oral delivery of SRF.
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页码:761 / 768
页数:7
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