Oral administration of PET tracers: Current status

Giordana Salvi de Souza; Dimitri B A Mantovani; Pascalle Mossel; Bartholomeus C M Haarman; Ana Maria Marques da Silva; Hendrikus H Boersma; Cristiane R G Furini; Adriaan A Lammertsma; Charalampos Tsoumpas; Gert Luurtsema

doi:10.1016/j.jconrel.2023.04.008

Oral administration of PET tracers: Current status

J Control Release. 2023 May:357:591-605. doi: 10.1016/j.jconrel.2023.04.008. Epub 2023 Apr 23.

Affiliations

¹ School of Medicine, PUCRS, Porto Alegre, Brazil; Medical Image Computing Laboratory, School of Technology, PUCRS, Porto Alegre, Brazil; Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands.
² Medical Image Computing Laboratory, School of Technology, PUCRS, Porto Alegre, Brazil; Hospital das Clinicas HCFMUSP, Faculdade de Medicina, Universidade de Sao Paulo, Sao Paulo, Brazil.
³ Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands.
⁴ Department of Psychiatry, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands.
⁵ Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands; Department of Clinical Pharmacy and Pharmacology, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands.
⁶ School of Medicine, PUCRS, Porto Alegre, Brazil; Laboratory of Cognition and Memory Neurobiology, Brain Institute, PUCRS, Porto Alegre, Brazil.
⁷ Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands. Electronic address: g.luurtsema@umcg.nl.

PMID: 37031742
DOI: 10.1016/j.jconrel.2023.04.008

Abstract

The oral route is the most widely used and preferable way of drug administration. Several pharmacokinetic processes play a role in the distribution of administered drugs. Therefore, accurate quantification of absorption, distribution, metabolism, excretion, and characterisation of drug kinetics after oral administration is extremely important for developing new human drugs. In vivo methods, such as gamma-scintigraphy, magnetic resonance imaging (MRI), and positron emission tomography (PET), have been used to analyse gastrointestinal tract (GIT) absorption behaviour. This scoping review provides an overview of PET studies that used oral tracer administration. A systematic literature search was performed using PubMed, EMBASE, Scopus, Science Direct, and Web of Science databases. Extensive variation between these studies was seen concerning acquisition protocols, quantification methods, and pharmacokinetic outcome parameters. Studies in humans indicate that it takes 10 to 30 min for the tracer to be in the intestine and about 100 min to reach its maximum concentration in the brain. In rodent studies, different pharmacokinetic parameters for the brain, blood, and GIT were estimated, showing the potential of PET to measure the absorption and distribution of drugs and pharmaceuticals non-invasively. Finally, regarding radiation protection, oral administration has a higher absorbed dose in GIT and, consequently, a higher effective dose. However, with the recent introduction of Long Axial Field of View (LAFOV) PET scanners, it is possible to reduce the administered dose, making oral administration feasible for routine clinical studies.

Keywords: Gastrointestinal tract; Oral administration; Pharmacokinetics; Positron emission tomography.

Publication types

Review
Research Support, Non-U.S. Gov't

MeSH terms

Administration, Oral
Brain* / diagnostic imaging
Gastrointestinal Tract / diagnostic imaging
Humans
Positron-Emission Tomography*