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Sci. Pharm. 2008, 76(2), 151-170; doi:10.3797/scipharm.0804-07 (registering DOI)

Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates

1
Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), P.O.Box: 31485-498, Karaj, Iran
2
Islamic Azad University, Science and Research Unit, P.O.Box: 14155-775, Tehran, Iran
*
Author to whom correspondence should be addressed.
Received: 6 April 2008 / Accepted: 15 May 2008 / Published: 18 May 2008
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Abstract

In order to use Auger-electron therapeutic effects in CD20 antigen targeting in lymphomas, Mabthera™ (rituximab) was successively labeled with [111In]-indium chloride (185 MBq) after conjugation with freshly prepared macrocyclic bifunctional chelating agent, N-succinimidyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA-NHS) and ccDTPA separately. Conjugated-Rituximab was obtained by the addition of 1 ml of a rituximab pharmaceutical solution (5 mg/ml, in phosphate buffer, pH=7.8) to a glass tube pre-coated with freshly prepared DOTA-NHS or ccDTPA (0.01-0.1 mg) at 25°C. Radiolabeling was performed at 37°C in 3h and room temperature for one hour for DOTA-conjugate and DTPA-conjugate respectively. HPLC showed an overall radiochemical purity of 97.5 and 95% for DOTA and DTPA-conjugates respectively (Specific activity =2800-5600 GBq/mM). The final isotonic 111In-rituximab complexes were checked by gel electrophoresis for radiolysis. Preliminary biodistribution studies in normal rat model performed to determine radioimmunoconjugates distribution of up to 48h.
Keywords: Rituximab; Indium-111; Biodistribution; Radiolabeling; Targetted Therapy Rituximab; Indium-111; Biodistribution; Radiolabeling; Targetted Therapy
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

JALILIAN, A.R.; SARDARI, D.; KIA, L.; ROWSHANFARZAD, P.; GAROUSI, J.; AKHLAGHI, M.; SHANEHSAZZADEH, S.; MIRZAII, M. Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates. Sci. Pharm. 2008, 76, 151-170.

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