Assistant Prof. Dr. Ismail Taha Ibrahim
Abstract
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.
KeywordsHaloperidol · 125I · Chloramine-T · Microemulsion · Biodistribution · Brain imaging
