biostudies-literatureMizutani AShin Nippon Biomedical Laboratories, Ltd.Grant-in-Aid for Scientific Research from the Japan Society for the Promotion of Science1026https://www.ebi.ac.uk/biostudies/studies/S-EPMC9145277biostudies-literatureUnknown14(5)Single-photon emission computed tomography (SPECT) imaging using intravenous radioactive ligand administration to indirectly evaluate the time-dependent effect of intranasal drugs with poor blood-brain barrier permeability on brain drug distributions in mice was evaluated. The biodistribution was examined using domperidone, a dopamine D2 receptor ligand, as the model drug, with intranasal administration at 0, 15, or 30 min before intravenous [¹²³I]IBZM administration. In the striatum, [¹²³I]IBZM accumulation was significantly lower after intranasal (IN) domperidone administration than in controls 15 min after intravenous [¹²⁵I]IBZM administration. [¹²³I]IBZM SPECT was acquired with intravenous (IV) or IN domperidone administration 15 min before [PharmaceuticsIndirect SPECT Imaging Evaluation for Possible Nose-to-Brain Drug Delivery Using a Compound with Poor Blood-Brain Barrier Permeability in Mice.PMC91452770118K19508 and 21H02865Nishii RKawai KSasaki KTorikai YFukakusa SSuzuki CMagata YMuranaka YOhuchi MKobayashi MHaruta SMizutani AfalseIndirect SPECT Imaging Evaluation for Possible Nose-to-Brain Drug Delivery Using a Compound with Poor Blood-Brain Barrier Permeability in Mice.Single-photon emission computed tomography (SPECT) imaging using intravenous radioactive ligand administration to indirectly evaluate the time-dependent effect of intranasal drugs with poor blood-brain barrier permeability on brain drug distributions in mice was evaluated. The biodistribution was examined using domperidone, a dopamine D2 receptor ligand, as the model drug, with intranasal administration at 0, 15, or 30 min before intravenous [¹²³I]IBZM administration. In the striatum, [¹²³I]IBZM accumulation was significantly lower after intranasal (IN) domperidone administration than in controls 15 min after intravenous [¹²⁵I]IBZM administration. [¹²³I]IBZM SPECT was acquired with intravenous (IV) or IN domperidone administration 15 min before [2022-01-01T00:00:00Z2022 May2025-04-22T18:21:51.093Z2025-04-06T02:22:58.043ZS-EPMC91452773563161110.3390/pharmaceutics14051026