Formulation of 68Ga BAPEN kit for myocardial positron emission tomography imaging and biodistribution study
Received 7 May 2009; received in revised form 7 October 2009; accepted 23 October 2009. published online 30 November 2009.
Abstract
Introduction
Tris(4,6-dimethoxysalicylaldimine)-N,N′-bis(3-aminopropyl)-N,N′-ethylenediamine (BAPEN), a tris(salicylaldimine) derivative, is a heart positron emission tomography (PET) agent when labeled with 68Ga. However, its labeling requires complicated and time-consuming procedures. In this study, the authors formulated a new BAPEN kit for convenient 68Ga labeling.
Methods
BAPEN (0.25 mg) kits were prepared by dispensing its solution in 1 M sodium acetate buffer (pH 5.5) into sterile vials and lyophilization. The prepared kits were labeled with generator-eluted 68Ga in 0.1 N HCl. Stability in human serum was tested. Expiration date was determined by accelerated testing according to US Food and Drug Administration guidelines. A Biodistribution study was performed in normal mice after injection via tail vein.
Results
The prepared kits achieved radiolabeling efficiencies in excess of 95% and showed a shelf-life of 98 days at 25°C and 64.3 months at 4°C. 68Ga-BAPEN was found to be stable in human serum at 37°C for at least 1 h. Furthermore, a biodistribution study revealed high heart uptake (10.8% ID/g, 1 h).
Conclusions
The authors developed a BAPEN kit for convenient labeling with 68Ga. The 68Ga-BAPEN showed high stability and excellent biodistribution results in normal mice, which is required for myocardial PET imaging.
aDepartment of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, 110-744 Seoul, South Korea
bCancer Research Institute, Seoul National University College of Medicine, Seoul 110-744, South Korea
cDepartment of Radiation Applied Life Science, Seoul National University College of Medicine, Seoul 110-744, South Korea
Corresponding author. Department of Nuclear Medicine, Seoul National University Hospital, Seoul 110-744, South Korea. Tel.: +82 2 2072 3805; fax: +82 2 745 7690.
ABSTRACT