Formulation of 68Ga BAPEN kit for myocardial positron emission tomography imaging and biodistribution study.
BACKGROUND
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 (68)Ga. However, its labeling requires complicated and time-consuming procedures. In this study, the authors formulated a new BAPEN kit for convenient (68)Ga 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 (68)Ga 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 degrees C and 64.3 months at 4 degrees C. (68)Ga-BAPEN was found to be stable in human serum at 37 degrees 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 (68)Ga. The (68)Ga-BAPEN showed high stability and excellent biodistribution results in normal mice, which is required for myocardial PET imaging.
Yang
Bo Yeun
BY
Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, 110-744 Seoul, South Korea.
Jeong
Jae Min
JM
Kim
Young Joo
YJ
Choi
Jae Yeon
JY
Lee
Yun-Sang
YS
Lee
Dong Soo
DS
Chung
June-Key
JK
Lee
Myung Chul
MC
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D005029:Ethylenediamines / Q000138:chemical synthesis / Q000302:isolation & purification / Q000493:pharmacokinetics*; D006321:Heart / Q000000981:diagnostic imaging*; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000302:isolation & purification / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography
D005029:Ethylenediamines; D009942:Organometallic Compounds; C081867:gallium bis(4,6-dimethoxy)salicylaldimine N,N'-bis(3-aminopropyl)ethylenediamine