PRELIMINARY EVALUATION OF AN ANTHRAQUINONE CONJUGATED DOTA DERIVATIVE AS SPECT AGENT

Authors

  • Anupriya Adhikari Institute of Nuclear Medicine and Allied Sciences, DRDO, Brigd. S K Mazumdar Road, Timarpur, Delhi-110054, INDIA Kanya Gurukul Campus, Gurukul Kangri Vishwavidyalaya, Haridwar-249404, Uttarakhand
  • Anupama Datta Institute of Nuclear Medicine and Allied Sciences, DRDO, Brigd. S K Mazumdar Road, Timarpur, Delhi-110054, INDIA
  • Krishna Chuttani Institute of Nuclear Medicine and Allied Sciences, DRDO, Brigd. S K Mazumdar Road, Timarpur, Delhi-110054, INDIA
  • Harish Rawat Institute of Nuclear Medicine and Allied Sciences, DRDO, Brigd. S K Mazumdar Road, Timarpur, Delhi-110054, INDIA
  • Abha Shukla Kanya Gurukul Campus, Gurukul Kangri Vishwavidyalaya, Haridwar-249404, Uttarakhand
  • Anil K. Mishra Institute of Nuclear Medicine and Allied Sciences, DRDO, Brigd. S K Mazumdar Road, Timarpur, Delhi-110054, INDIA

Keywords:

Anthraquinone, Tumor, Single Photon Emission Computed Tomography

Abstract

Objective: An anthraquinone derivative, DO3A-Act-AQ having DO3A (1, 4, 7, 10-tetraazacyclododecane-1, 4, 7-trisacetic acid) scaffold is radio labeled with 99mTc radioisotope and evaluated as a SPECT imaging agent for tumor.

Methods: Preliminary in-vivo evaluation of 99mTc-DO3A-Act-AQ radioconjugate including blood kinetics, biodistribution and gamma scintigraphic imaging is performed on BMG-1 tumor xenografted mice after successful optimization of the radiolabeling condition.

Results: The radiotracer, 99mTc-DO3A-Act-AQ was produced in high radiochemical yield of>96% and specific activity of 3.62 MBq/nmol at pH 7.5 and 150 µg stannous chloride. Radioconjugate displayed excellent in-vitro and in-vivo stability with only ~2% transchelation of radiometal at 24 h p. i and rapid blood clearance from the system with t1/2(F) = 38.04±0.35 min and t1/2(S) = 5 h 30 min±0.67. Significant tumor-to-muscle ratio of>7 at 2 h p. i. in biodistribution and SPECT imaging studies in BMG-1 tumor xenografted mice suggested the tumor specificity of the radioconjugate.

Conclusion: Stable radiocomplex formation of 99mTc-DO3A-Act-AQ and its significant tumor specificity demonstrated its future application as a promising SPECT radioligand for tumor imaging.

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Author Biography

Abha Shukla, Kanya Gurukul Campus, Gurukul Kangri Vishwavidyalaya, Haridwar-249404, Uttarakhand

Department of Chemistry

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Published

01-04-2015

How to Cite

Adhikari, A., A. Datta, K. Chuttani, H. Rawat, A. Shukla, and A. K. Mishra. “PRELIMINARY EVALUATION OF AN ANTHRAQUINONE CONJUGATED DOTA DERIVATIVE AS SPECT AGENT”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 4, Apr. 2015, pp. 85-89, https://mail.innovareacademics.in/journals/index.php/ijpps/article/view/4821.

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