Neuroprotective study of Nigella sativa-loaded oral provesicular lipid formulation: in vitro and ex vivo study

Drug Deliv. 2014 Sep;21(6):487-94. doi: 10.3109/10717544.2014.886640. Epub 2014 Mar 7.

Abstract

Aim: The aim of this research was to develop proniosome (niosomes) of Nigella sativa (NS) to improve its drug release, gastrointestinal (GI) permeation and neuroprotective activity.

Materials and methods: Proniosomes were prepared by thin film method using various compositions of nonionic surfactants, cholesterol, and phosphatidylcholine. The optimum influence of different formulation variables of NS such as surfactant type, phosphatidylcholine and cholesterol concentration were optimized for size and entrapment efficiency.

Results and discussion: Results indicated that prepared niosome showed smaller size with high entrapment efficiency. The permeation enhancement ratio was found to be 2.16 in comparison to control with maximum flux value obtained was 7.23 µg/cm(2)/h for formulation NS6. The in vivo study revealed that the niosomal dispersion significantly improved neuroprotective activity in comparison to standard and control formulation.

Conclusion: In conclusion, developed proniosomal formulation could be one of the promising delivery system for NS with better drug release and GI permeation profiles and improved neuroprotective activity and merits for further study.

Keywords: Lipid formulation; Nigella Sativa; neuroprotective; oral.

MeSH terms

  • Administration, Oral
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Cholesterol / chemistry
  • Gastrointestinal Absorption / physiology
  • Gastrointestinal Tract / metabolism
  • Lipids / chemistry*
  • Lipids / pharmacology*
  • Liposomes / chemistry
  • Liposomes / metabolism
  • Liposomes / pharmacology
  • Neuroprotective Agents / chemistry*
  • Neuroprotective Agents / metabolism
  • Neuroprotective Agents / pharmacology*
  • Nigella sativa / chemistry*
  • Particle Size
  • Permeability
  • Phosphatidylcholines / chemistry
  • Rats
  • Rats, Wistar
  • Surface-Active Agents / chemistry

Substances

  • Lipids
  • Liposomes
  • Neuroprotective Agents
  • Phosphatidylcholines
  • Surface-Active Agents
  • Cholesterol