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Production of [103Pd]Bleomycin complex for targeted therapy

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Języki publikacji
EN
Abstrakty
EN
Due to the anticancer properties of bleomycin (BLM) complexes, production of [103Pd]bleomycin ([103Pd]BLM) was targeted. Palladium-103 (T1/2 = 16.96 d) was produced via the 103Rh(p,n)103Pd nuclear reaction using a natural rhodium target. Proton energy was 18 MeV with 200 mA irradiation for 15 h (final activity 25.9 GBq of 103Pd2+, RCP > 95%, radionuclidic purity > 99%). 103Pd was separated from the irradiated target by anion exchange using a Dowex 1´8 (Cl-)/100-200 mesh resin in the form of Pd(NH3)2Cl2 in order to react with bleomycin to yield [103Pd]BLM. Chemical purity of the final product was in accordance to the accepted limits. [103Pd]BLM was prepared with a radiochemical yield of more than 98% at 80°C in 30 min. The labeling reaction was optimized for time, temperature and ligand concentration. Radiochemical purity of more than 99% was obtained using RTLC with specific activity of about 370 MBq/mmol. The stability of the tracer was checked in the final product and presence of human serum at up to 3 h. The complex was stable in human serum at 37°C up to 2 h of incubation. Biodistribution studies using a SPECT system performed in normal rats in the first 2-3 h.
Czasopismo
Rocznik
Strony
119--123
Opis fizyczny
Bibliogr. 21 poz., rys.
Twórcy
autor
autor
  • Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), Moazzen Blvd., Rajaee shahr, Karaj, Iran, P. O. Box 31485-498, Tel./Fax: +98 261 4436397, ajalilian@nrcam.org
Bibliografia
  • 1. Albertini JP, Garnier-Suillerot A (1986) Evidence of the complexation of the antitumor drug bleomycin with cis-[diaminedichloroplatinum] and with palladium derivatives. Physicochemical characteristics, interaction with DNA, and antitumor activity. Inorg Chem 25:1216−1221
  • 2. Brooks RC, Carnochan P, Vollano JF et al. (1999) Metal complexes of bleomycin: Evaluation [Rh-105]-bleomycin for use in targeted radiotherapy. Nucl Med Biol 26:421−430
  • 3. Grove RB, Eckelman WC, Reba RC (1974) Distribution of the labeled bleomycin in normal and tumor-bearing mice. J Nucl Med 15:917−919
  • 4. Hoehn ST, Junker HD, Bunt RC, Turner CJ, Stubbe J (2001) Solution structure of Co(III)-bleomycin-OOH bound to a phosphoglycolate lesion containing oligonucleotide: Implications for bleomycin-induced double-strand DNA cleavage. Biochemistry 22:5894−5905
  • 5. Jaaskela-Saari HA, Kairemo KJ, Ramsay HA, Grenman R (1998) Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines.Int J Radiat Biol 73:565−570
  • 6. Jalilian AR, Fateh B, Ghergherehchi M et al. (2003)Preparation, distribution, stability and tumor imaging properties of [62Zn]Bleomycin in normal and tumorbearing mice. Iran J Radiat Res 1:37−44
  • 7. Jalilian AR, Rowshanfarzad P, Sabet M, Novinrooz A,Raisali G (2005) Preparation of [66Ga]Bleomycin complex as a possible PET radiopharmaceutical. J Radioanal Nucl Chem 264:617−621
  • 8. Kahn PC, Milunsky C, Devanjee MK, Rudders RA (1977)The place of 57Co-bleomycin scanning in the evaluation of the tumors. Am J Roentgenol 129:267−273
  • 9. Kairemo KJ, Ramsay HA, Tagesson M (1997) Indium-111 bleomycin complex for radiochemotherapy of head and neck cancer-dosimetric and biokinetic aspect. Eur J Nucl Med 23:631−638
  • 10. Meigooni AS, Zhang H, Perry C, Dini SA, Koona RA (2003) Theoretical and experimental determination of dosimetric characteristics for brachy seed Pd-103, model Pd-1. Appl Radiat Isot 58:533−541
  • 11. Neirincky RD (1977) Excitation function for the 60Ni(a,2n)62Zn reaction and production of 62Znbleomycin.Int J Appl Radiat Isot 28:808−809
  • 12. Papakyriakou AI, Bratsos N, Katsarus S (2003) Structural studies on metallobleomycins: the interaction of Pt and Pd with bleomycins. J Serb Chem Soc 68:337−348
  • 13. Sadeghi M, Van den Winkel P, Afarideh H, Haji-Saeid M (2004) A thick rhodium electrodeposition on copper backing as the target for production of palladium-103.J Radioanal Nucl Chem 262:665−672
  • 14. Sherertz T, Wallner K, Merrick G et al. (2004) The prognostic significance of Gleason pattern 5 in prostate cancer patients treated with Pd-103 plus beam radiation therapy. Cancer J 10:301−306
  • 15. Stern PH, Halpern SE, Hagan PL, Howell SB, Dabbs JE, Gordon RM (1981) Cytotoxic activity, tumor accumulation and tissue distribution of ruthenium-103-labeled-bleomycin. J Nat Cancer Inst 66:807−811
  • 16. Sudar S, Cserpak F, Qaim SM (2002) Measurements and nuclear model calculations on proton-induced reactions on 103Rh up to 40 MeV: Evaluation of the excitation function of the 103Rh(p,n)103Pd reaction relevant to the production of the therapeutic radionuclide 103Pd. Appl Radiat Isot 56:821−831
  • 17. Takita T, Umezawa Y, Saito SI et al. (1982) Total synthesis of bleomycin A2. Tetrahedron Lett 123:521−524
  • 18. Thakur ML (1973) The preparation of indium-111 labelled bleomycin for tumour localisation. Int J Appl Radiat Isot 21:654−659
  • 19. Umezawa H, Suhara Y, Takita T, Maeda K (1966) Purification of bleomycins. J Antibiot (Tokyo) 19:210−215
  • 20. Umezawa H, Takeuchi S, Hori T, Sawa M (1972) Studies on the mechanism of antitumor effect of bleomycin of squamous cell carcinoma. J Antibiot (Tokyo) 7:409−420
  • 21.United States Pharmacopeiae (2005) NF 23, USP 28,[201Tl]Thallous chloride monograph, p 1895
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BUJ6-0004-0017
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