This study aims to develop a novel
68
Ga-labeled
tracer,
which can covalently bind to albumin in vivo based on the maleimide–thiol
strategy, and to evaluate its potential applications using positron
emission tomography (PET).
68
Ga-labeled maleimide-monoamide-DOTA
(denoted as [
68
Ga]Ga-DM) was prepared conveniently with
a high radiochemical yield (>90%) and radiochemical purity (>99%).
Its molar activity was calculated as 249.60 ± 68.50 GBq/μmol,
and the octanol–water partition coefficient (Log
P
) was −3.15 ± 0.08 with good stabilities. In vitro experiments
showed that [
68
Ga]Ga-DM can bind to albumin efficiently
and rapidly, with a binding fraction of over 70%. High uptake and
excellent retention in blood were observed with a long half-life (
t
1/2Z
) of 190.15 ± 24.14 min, which makes
it possible for blood pool PET imaging with high contrast. The transient
micro-bleeding in the rat model was detected successfully with PET
imaging. In addition, the uptakes of [
68
Ga]Ga-DM in the
inflammatory popliteal lymph nodes depend on the severity (5.90% ID/g
and 2.32% ID/g vs 1.01% ID/g for healthy lymph nodes at 0.5 h post-injection)
indicating its feasibility for lymphatic imaging. In conclusion, a
novel
68
Ga-labeled tracer was prepared with high efficiency
and yield in mild conditions. Based on the promising properties of
bonding covalently to albumin, great stability, high blood contrast
with a long half-life, and well environmental tolerance, [
68
Ga]Ga-DM could be developed as a potential tracer for PET imaging
of blood pool, bleeding, and vascular permeability alteration diseases
in the clinic.