Intranasal drug delivery of iodo-haloperidol as a radiopharmaceutical brain imaging agent
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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
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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.
- 6.Stephen MM, Chester AM, Kathleen MB, Thomas FB (1987) Synthesis and in vivo evaluation of 122I- and 131I-labelled iodoperidol, a potential agent for the tomographic assessment of cerebral perfusion. Nucl Med Biol 14:91–98Google Scholar
- 9.Motaleb MA, Ibrahim IT, Sayyed ME, Awad G (2017) 131I-trazodone: preparation, quality control and in vivo biodistribution study by intranasal and intravenous routes as a hopeful brain imaging radiopharmaceutical. Rev Esp Med Nucl Imagen Mol 36:371–376Google Scholar
- 10.Walovitch RC, Hill TC, Garrity ST, Cheesman EH, Burgess BA, O’Leary DH et al (1989) Characterization of Technetium-99m-L, L-ECD for brain perfusion imaging, part 1: pharmacology of technetium-99m ECD in nonhuman primates. J Nucl Med 30:1892–1901Google Scholar
- 11.Neirinckx RD, Canning LR, Piper IM, Nowotnik DP, Pickett RD, Holmes RA et al (1987) Technetium-99m d, l-HM-PAO: a new radiopharmaceutical for SPECT imaging of regional cerebral blood perfusion. J Nucl Med 28:191–202Google Scholar
- 15.Kassis AI (2003) Cancer therapy with auger electrons: Are we almost there? J Nucl Med 44:1479–1481Google Scholar
- 18.Rasal A, Mahajan HS, Shaikh HT, Surana SJ (2010) Development and characterization of nasal mucoadhesive microemulsion of sumatriptan succinate. IJNDD 2:103–108Google Scholar
- 20.Rashed HM, Shamma RN, Basalious EB (2017) Contribution of both olfactory and systemic pathways for brain targeting of nimodipine-loaded lipo-pluronics micelles: in vitro characterization and in vivo biodistribution study after intranasal and intravenous delivery. Drug Deliv 24:181–187CrossRefGoogle Scholar
- 26.Sanad MH, Salama DH, Marzook FA (2016) Radioiodinated famotidine as a new highly selective radiotracer for peptic ulcer disorder detection, diagnostic nuclear imaging and biodistribution. Radiochim Acta 105:389–398Google Scholar
- 27.Attila V, Sandor N, Zoltan K, Rezso GL, Rosch F (2011) Handbook of nuclear chemistry, 2nd edn. Springer, New YorkGoogle Scholar