International Journal of Nanomedicine 2015-01-01

Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement.

Rong Lu, Shan Liu, Qilin Wang, Xia Li

文献索引：Int. J. Nanomedicine 10 , 4937-46, (2015)

全文：HTML全文

摘要

Oral administration remains a significant challenge in regards to drugs with serious solubility and stability issues. This article aimed to investigate the suitability of nanoemulsions as oral carriers of stiripentol (STP), an acid-labile drug, for enhancement of stability and bioavailability. STP-loaded nanoemulsions (STP-NEs) were prepared by using a solvent-diffusion/ultrasonication technique. STP-NEs were characterized in a variety of ways such as by particle size, entrapment efficiency, in vitro drug release, and transmission electron microscopy. A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit). The resultant nanoemulsions were 146.6 nm in particle size with an entrapment efficiency of 99.47%. It was demonstrated that nanoemulsions significantly improved the biochemical stability and bioavailability of STP. The bioavailability of STP-NEs was up to 206.2% relative to Diacomit. Nanoemulsions fabricated from poly(ethylene glycol) monooleate/medium-chain triglycerides exhibited excellent performance in drug stabilization and absorption enhancement. The results suggest that STP-NEs are a promising means to solve the problems associated with stability and solubility of STP.

相关化合物

  • 甲醇
  • N-水杨酰色胺
  • 双氯芬酸钠

相关文献：

BBS4 directly affects proliferation and differentiation of adipocytes.

2014-09-01

[Cell. Mol. Life Sci. 71(17) , 3381-92, (2014)]

Urinary metabolic fingerprinting of mice with diet-induced metabolic derangements by parallel dual secondary column-dual detection two-dimensional comprehensive gas chromatography.

2014-09-26

[J. Chromatogr. A. 1361 , 265-76, (2014)]

Biomolecular imaging with a C60-SIMS/MALDI dual ion source hybrid mass spectrometer: instrumentation, matrix enhancement, and single cell analysis.

2014-11-01

[J. Am. Soc. Mass Spectrom. 25(11) , 1897-907, (2014)]

Synergistic activity of tenofovir and nevirapine combinations released from polycaprolactone matrices for potential enhanced prevention of HIV infection through the vaginal route.

2014-10-01

[Eur. J. Pharm. Biopharm. 88(2) , 406-14, (2014)]

Antinematode activity of Violacein and the role of the insulin/IGF-1 pathway in controlling violacein sensitivity in Caenorhabditis elegans.

2014-01-01

[PLoS ONE 9(10) , e109201, (2014)]

更多文献...