Self-nanoemulsifying drug-delivery systems improve oral absorption and antischistosomal activity of epiisopiloturine

Nanomedicine (Lond). 2018 Apr 1;13(7):689-702. doi: 10.2217/nnm-2017-0308. Epub 2018 Mar 22.

Abstract

Aim: To develop a self-nanoemulsifying drug-delivery system (SNEDDS) able to improve oral absorption of epiisopiloturine (EPI), and test the antischistosomal activity in a mice model.

Results: SNEDDS had a nanoscopic size and was able to enhance EPI bioavailability after oral administration, and SNEDDS-EPI (40 mg.kg-1) improved the in vivo antischistosomal activity of EPI, demonstrating that SNEDDS was able to improve the pharmacokinetics of EPI, and to maintain the pharmacodynamic activity against Schistosoma mansoni in vivo.

Conclusion: Taken together, these results indicate that SNEDDS-EPI is efficient in reducing worm burden in comparison to treatment with the free version of EPI. [Formula: see text].

Keywords: antischistosomal activity; oral absorption; self-nanoemulsifying drug-delivery systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Butyrolactone / administration & dosage
  • 4-Butyrolactone / analogs & derivatives*
  • 4-Butyrolactone / chemistry
  • 4-Butyrolactone / pharmacokinetics
  • Administration, Oral
  • Animals
  • Biological Availability
  • Disease Models, Animal
  • Drug Delivery Systems*
  • Emulsions / administration & dosage
  • Emulsions / chemistry
  • Humans
  • Imidazoles / administration & dosage*
  • Imidazoles / chemistry
  • Imidazoles / pharmacokinetics
  • Mice
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Particle Size
  • Schistosoma mansoni / drug effects
  • Schistosoma mansoni / pathogenicity
  • Schistosomiasis mansoni / drug therapy*
  • Schistosomiasis mansoni / parasitology
  • Solubility

Substances

  • Emulsions
  • Imidazoles
  • epiisopiloturine
  • 4-Butyrolactone