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Volume 76
Issue 2
10.3797/scipharm.0804-07
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Article

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

by
Amir R. JALILIAN
1,*,
Darush SARDARI
2,
Leila KIA
2,
Pejman ROWSHANFARZAD
1,
Javad GAROUSI
1,
Mehdi AKHLAGHI
1,
Saeed SHANEHSAZZADEH
1 and
Mohammad MIRZAII
1
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.
Sci. Pharm. 2008, 76(2), 151-170; https://doi.org/10.3797/scipharm.0804-07
Submission received: 6 April 2008 / Accepted: 15 May 2008 / Published: 18 May 2008
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.0804-07

AMA Style

JALILIAN AR, 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. Scientia Pharmaceutica. 2008; 76(2):151-170. https://doi.org/10.3797/scipharm.0804-07

Chicago/Turabian Style

JALILIAN, Amir R., Darush SARDARI, Leila KIA, Pejman ROWSHANFARZAD, Javad GAROUSI, Mehdi AKHLAGHI, Saeed SHANEHSAZZADEH, and Mohammad MIRZAII. 2008. "Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates" Scientia Pharmaceutica 76, no. 2: 151-170. https://doi.org/10.3797/scipharm.0804-07

APA Style

JALILIAN, A. R., SARDARI, D., KIA, L., ROWSHANFARZAD, P., GAROUSI, J., AKHLAGHI, M., SHANEHSAZZADEH, S., & MIRZAII, M. (2008). Preparation, Quality Control and Biodistribution Studies of two [111In]-Rituximab Immunoconjugates. Scientia Pharmaceutica, 76(2), 151-170. https://doi.org/10.3797/scipharm.0804-07

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