Spontaneous emulsification of nifedipine-loaded self-nanoemulsifying drug delivery system

AAPS PharmSciTech. 2015 Apr;16(2):435-43. doi: 10.1208/s12249-014-0238-0. Epub 2014 Oct 31.

Abstract

Self-nanoemulsifying drug delivery system (SNEDDS) can be used to improve dissolution of poorly water-soluble drugs. The objective of this study was to prepare SNEDDS by using ternary phase diagram and investigate their spontaneous emulsifying property, dissolution of nifedipine (NDP), as well as the pharmacokinetic profile of selected SNEDDS formulation. The results showed that the composition of the SNEDDS was a great importance for the spontaneous emulsification. Based on ternary phase diagram, the region giving the SNEDDS with emulsion droplet size of less than 300 nm after diluting in aqueous medium was selected for further formulation. The small-angle X-ray scattering curves showed no sharp peak after dilution at different percentages of water, suggesting non-ordered structure. The system was found to be robust in different dilution volumes; the droplet size was in nanometer range. In vitro dissolution study showed remarkable increase in dissolution of NDP from SNEDDS formulations compared with NDP powders. The pharmacokinetic study of selected SNEDDS formulation in male Wistar rats revealed the improved maximum concentration and area under the curve. Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Emulsions / chemistry*
  • Male
  • Nanoparticles / chemistry*
  • Nifedipine / chemistry*
  • Particle Size
  • Rats
  • Rats, Wistar
  • Solubility
  • Surface-Active Agents / chemistry

Substances

  • Drug Carriers
  • Emulsions
  • Surface-Active Agents
  • Nifedipine