Intranasal drug delivery of iodo-haloperidol as a radiopharmaceutical brain imaging agent

  • M. E. SayedEmail author
  • M. A. Motaleb
  • I. T. Ibrahim
  • G. A. S. Awad
  • R. O. Ahmed


Haloperidol (HP) is a dopamine blocking agent. HP was radiolabeled with 125I using direct electrophilic substitution. Different HP formulations such as intravenous solution (VS), intranasal solution (NS) and intranasal microemulsion (NME) have been prepared. Optimum labeling yield of 125I-HP was obtained 93.42 ± 1.53%. Isopropylmyristate oil (10%), Tween 80 (30%), propylene glycol (15%) and aqueous phase (45%) were used for NME preparation. Using Swiss Albino mice, the % brain uptake were 1.4 ± 0.2, 4.3 ± 0.2 and 5.7 ± 0.4% for VS, NS and NME, respectively. 125I-HP in NME formula showed superiority as drug delivery system for brain imaging.


Haloperidol 125Chloramine-T Microemulsion Biodistribution Brain imaging 


Compliance with ethical standards

Conflict of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript.


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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2018

Authors and Affiliations

  1. 1.Radio Labeled Compounds Department, Hot Labs CentreEgyptian Atomic Energy AuthorityCairoEgypt
  2. 2.Department of Pharmaceutics and Industrial Pharmacy, Faculty of PharmacyAin Shams UniversityCairoEgypt
  3. 3.Faculty of PharmacyAlbayan UniversityBaghdadIraq

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