کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
11020258 | 1717600 | 2019 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Single vial cold kits optimized for preparation of gastrin releasing peptide receptor (GRPR)-radioantagonist 68Ga-RM2 using three different 68Ge/68Ga generators
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
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چکیده انگلیسی
68Ga-RM2 is a gastrin releasing peptide receptor (GRPR) antagonist PET (positron emission tomography) radiotracer which is being investigated in clinical trials as a potential prostate cancer imaging agent. Simple, one-step kit formulation of 68Ga-RM2 would facilitate multicentre trials and allow easier integration in hospital radiopharmacy. Herein we report development of three sets of single-vial RM2 cold kits validated for formulation with three respective 68Ge/68Ga generators eluted in 0.6âM, 0.1âM and 0.05âM HCl (hydrochloric acid). Cold kits of varied pH (2, 3, 4 and 5) were prepared using 2âM sodium acetate for three different 68Ge/68Ga generators to determine influence of pH on the radiochemical yield of 68Ga-RM2. Buffer content was optimized with respect to volume of 68GaCl3 eluate to be added (1âmL/2âmL/ 5âmL). Sterility, apyrogenicity and long term stability of cold kits; in vitro and serum stability of 68Ga-RM2 were investigated. In vitro cellular uptake and inhibition studies were performed to demonstrate the specificity of kit-formulated 68Ga-RM2. The radiochemical yield of 68Ga-RM2 formulated from three different generators was observed to be maximum at pH 3 (99â±â0.5%). Cold kits stored for 6 months at 0â°C also resulted in high radiochemical yield. 68Ga-RM2 exhibited excellent in vitro stability (1âh) and serum stability (1âh). In vitro cellular uptake of 5â±â0.8% in PC3 cells with >85% inhibition was observed for the 68Ga-RM2 radiotracer indicating its specificity towards GRPR expression. These simple, robust kits shall allow hospitals with different generators to participate in clinical studies of 68Ga-RM2 for screening of GRPR-expressing prostate tumors.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 163, 30 January 2019, Pages 39-44
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 163, 30 January 2019, Pages 39-44
نویسندگان
Kusum Vats, Rohit Sharma, Mythili Kameswaran, Drishty Satpati, Ashutosh Dash,