In vivo characterisation of a therapeutically relevant self-assembling (18) F-labelled β-sheet forming peptide and its hydrogel using positron emission tomography.
AuthorsMorris, Olivia C
Williams, Kaye J
AffiliationWolfson Molecular Imaging Centre, Univ of Manchester
MetadataShow full item record
AbstractPositron emission tomography (PET) and fluorescence labelling have been used to assess the pharmacokinetics, biodistribution and eventual fate of a hydrogel-forming nonapeptide, FEFKFEFKK (F9), in healthy mice, using (18) F-labelled and fluorescein isothiocyanate (FITC)-labelled F9 analogues. F9 was site-specifically radiolabelled with 2-[(18) F]fluoro-3-pyridinecarboxaldehyde ([(18) F]FPCA) via oxime bond formation. [(18) F]FPCA-F9 in vivo fate was evaluated both as a solution, following intravenous administration, and as a hydrogel when subcutaneously injected. The behaviour of FITC-F9 hydrogel was assessed following subcutaneous injection. [(18) F]FPCA-F9 demonstrated high plasma stability and primarily renal excretion; [(18) F]FPCA-F9 when in solution and injected into the bloodstream displayed prompt bladder uptake (53.4 ± 16.6 SUV at 20 minutes postinjection) and rapid renal excretion, whereas [(18) F]FPCA-F9 hydrogel, formed by co-assembly of [(18) F]FPCA-F9 monomer with unfunctionalised F9 peptide and injected subcutaneously, showed gradual bladder accumulation of hydrogel fragments (3.8 ± 0.4 SUV at 20 minutes postinjection), resulting in slower renal excretion. Gradual disaggregation of the F9 hydrogel from the site of injection was monitored using FITC-F9 hydrogel in healthy mice (60 ± 3 over 96 hours), indicating a biological half-life between 1 and 4 days. The in vivo characterisation of F9, both as a gel and a solution, highlights its potential as a biomaterial.
CitationIn vivo characterisation of a therapeutically relevant self-assembling (18) F-labelled β-sheet forming peptide and its hydrogel using positron emission tomography. 2017, 60 (10):481-488 J Labelled Comp Radiopharm
JournalJournal of Labelled Compounds & Radiopharmaceuticals
- More advantages in detecting bone and soft tissue metastases from prostate cancer using <sup>18</sup>F-PSMA PET/CT.
- Authors: Pianou NK, Stavrou PZ, Vlontzou E, Rondogianni P, Exarhos DN, Datseris IE
- Issue date: 2019 Jan-Apr
- Development & automation of a novel [(18)F]F prosthetic group, 2-[(18)F]-fluoro-3-pyridinecarboxaldehyde, and its application to an amino(oxy)-functionalised Aβ peptide.
- Authors: Morris O, Gregory J, Kadirvel M, Henderson F, Blykers A, McMahon A, Taylor M, Allsop D, Allan S, Grigg J, Boutin H, Prenant C
- Issue date: 2016 Oct
- In vitro and in vivo evaluation of a (18)F-labeled high affinity NOTA conjugated bombesin antagonist as a PET ligand for GRPR-targeted tumor imaging.
- Authors: Varasteh Z, Aberg O, Velikyan I, Lindeberg G, Sörensen J, Larhed M, Antoni G, Sandström M, Tolmachev V, Orlova A
- Issue date: 2013
- Development of [<sup>18</sup>F]FAMTO: A novel fluorine-18 labelled positron emission tomography (PET) radiotracer for imaging CYP11B1 and CYP11B2 enzymes in adrenal glands.
- Authors: Bongarzone S, Basagni F, Sementa T, Singh N, Gakpetor C, Faugeras V, Bordoloi J, Gee AD
- Issue date: 2019 Jan - Feb
- Pilot pharmacokinetic and dosimetric studies of (18)F-FPPRGD2: a PET radiopharmaceutical agent for imaging α(v)β(3) integrin levels.
- Authors: Mittra ES, Goris ML, Iagaru AH, Kardan A, Burton L, Berganos R, Chang E, Liu S, Shen B, Chin FT, Chen X, Gambhir SS
- Issue date: 2011 Jul