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

Authors :
Wang, Haipeng
Wang, Huiyun
Yang, Wenlong
Yu, Mengjie
Sun, Shuilin
Xie, Baogang
Source :
AAPS PharmSciTech; Feb2018, Vol. 19 Issue 2, p761-768, 8p
Publication Year :
2018

Abstract

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 <italic>via</italic> 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
15309932
Volume :
19
Issue :
2
Database :
Complementary Index
Journal :
AAPS PharmSciTech
Publication Type :
Academic Journal
Accession number :
127734586
Full Text :
https://doi.org/10.1208/s12249-017-0901-3