Oral administration of PET tracers: Current status

• Published in: Journal of controlled release 2023-05, Vol.357, p.591-605
• Main Authors: Salvi de Souza, Giordana, Mantovani, Dimitri B.A., Mossel, Pascalle, Haarman, Bartholomeus C.M., Marques da Silva, Ana Maria, Boersma, Hendrikus H., Furini, Cristiane R.G., Lammertsma, Adriaan A., Tsoumpas, Charalampos, Luurtsema, Gert
• Format: Article
• Language: English
• Subjects: Administration, Oral; Brain - diagnostic imaging; Gastrointestinal tract; Gastrointestinal Tract - diagnostic imaging; Humans; Oral administration; Pharmacokinetics; Positron emission tomography
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2023.04.008

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. [Display omitted] •This route of administration results in delayed plasma peaks dependent on the tracer, population, fasting, use of anaesthetics, and GIT motility.•The approach can have clinical implications for therapeutic strategies, drug dosages, and the treatment of GIT diseases.