Intranasal nanoemulsion based brain targeting drug delivery system of risperidone

Int J Pharm. 2008 Jun 24;358(1-2):285-91. doi: 10.1016/j.ijpharm.2008.03.029. Epub 2008 Mar 27.


The objective of investigation was to prepare nanoemulsion containing risperidone (RSP) to accomplish the delivery of drug to the brain via nose. Risperidone nanoemulsion (RNE) and mucoadhesive nanoemulsion (RMNE) were characterized for drug content, pH, percentage transmittance, globule size and zeta potential. Biodistribution of RNE, RMNE, and risperidone solution (RS) in the brain and blood of Swiss albino rats following intranasal (i.n.) and intravenous (i.v.) administration was examined using optimized technetium labeled ((99m)Tc-labeled) RSP formulations. Gamma scintigraphy imaging of rat brain following i.v. and i.n. administrations were performed to ascertain the localization of drug in brain. The brain/blood uptake ratio of 0.617, 0.754, 0.948, and 0.054 for RS (i.n.), RNE (i.n.), RMNE (i.n.), and RNE (i.v.), respectively, at 0.5h are indicative of direct nose to brain transport bypassing the blood-brain barrier. Higher drug transport efficiency (DTE%) and direct nose to brain drug transport (direct transport percentage, DTP%) for mucoadhesive nanoemulsions indicated more effective and best brain targeting of RSP amongst the prepared nanoemulsions. Studies conclusively demonstrated rapid and larger extent of transport of RSP by RMNE (i.n.) when compared to RS (i.n.), RNE (i.n.) and RNE (i.v.) into the rat brain.

MeSH terms

  • Administration, Intranasal
  • Animals
  • Antipsychotic Agents / administration & dosage*
  • Antipsychotic Agents / pharmacokinetics
  • Area Under Curve
  • Brain / drug effects*
  • Drug Delivery Systems*
  • Emulsions
  • Female
  • Indicators and Reagents
  • Injections, Intravenous
  • Isotope Labeling
  • Male
  • Mice
  • Motor Activity / drug effects
  • Nanoparticles
  • Radiopharmaceuticals / chemistry
  • Rats
  • Risperidone / administration & dosage*
  • Risperidone / pharmacokinetics
  • Technetium / chemistry
  • Tissue Distribution


  • Antipsychotic Agents
  • Emulsions
  • Indicators and Reagents
  • Radiopharmaceuticals
  • Technetium
  • Risperidone