Internal radiotherapy and dosimetric study for 111In/177Lu-pegylated liposomes conjugates in tumor-bearing mice

Hsin Ell Wang, Hung Man Yu, Yi Ching Lu, Ning Ning Heish, Yun Long Tseng, Kuang Liang Huang, Kuo Tang Chuang, Chin Hsiung Chen, Jeng Jong Hwang, Wuu Jyh Lin, Shyh Jen Wang, Gann Ting, Jacqueline Whang-Peng, Win Ping Deng

Research output: Contribution to journalArticle

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Abstract

In vivo characterization and dosimetric analysis has been performed to evaluate the potential of pegylated liposomes as carriers of radionuclides in tumor internal radiotherapy. Methods: The DTPA/PEG-liposomes were synthesized with a medium size of 110 nm, conjugated with 111In/177Lu-(oxine)3 to afford 111In/177Lu-liposome. The stability of 111In/177Lu-liposome in serum was investigated. The biodistribution, scintigraphic imaging and pharmacokinetics of 111In/177Lu-liposomes after intravenous(i.v.) injection into C-26 tumor-bearing BALB/cByJ mice were studied. Radiation dose was estimated by MIRD-III program. Results: The incorporation efficiency of 111In/177Lu into liposomes was 95%. After incubation at 37 °C for 72 h in serum, more than 83% of radioactivity was still retained in the intact 111In/177Lu-liposomes. The biodistribution of 111In-liposomes showed that the radioactivity in the blood decreased from 23.14±8.16%ID/g at 1 h to 0.02±0.00%ID/g at 72 h post-injection (p.i.), while reaching its maximum accumulation in tumors at 48 h p.i., with half-life in blood of 10.2 h. The results were supported by that of 177Lu-liposomes. Scintigraphic imaging with 111In-liposomes showed unambiguous tumor images at 48 h p.i. Dose estimation showed that the absorbed dose in tumor from 177Lu-liposomes was 5.74×10-5 Gy/MBq. Conclusions: This study provides an in vivo characterization and dosimetric evaluation for the use of liposome systems as carriers in targeted radionuclide therapy. The results suggest that adequate tumor targeting as well as dose delivered to tumors could be achieved by the use of radionuclide targeted liposomes.

Original languageEnglish
Pages (from-to)533-537
Number of pages5
JournalNuclear Instruments and Methods in Physics Research, Section A: Accelerators, Spectrometers, Detectors and Associated Equipment
Volume569
Issue number2 SPEC. ISS.
DOIs
Publication statusPublished - Dec 20 2006

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Bearings (structural)
Liposomes
Radiotherapy
mice
Tumors
radiation therapy
tumors
radioactive isotopes
injection
dosage
radioactivity
serums
blood
Radioisotopes
Radioactivity
half life
Blood
therapy
Imaging techniques
Pharmacokinetics

Keywords

  • Dosimetry
  • Indium-111
  • Lutetium-177
  • Radiolabeled pegylated liposomes
  • Targeted radionuclide therapy

ASJC Scopus subject areas

  • Instrumentation
  • Nuclear and High Energy Physics

Cite this

Internal radiotherapy and dosimetric study for 111In/177Lu-pegylated liposomes conjugates in tumor-bearing mice. / Wang, Hsin Ell; Yu, Hung Man; Lu, Yi Ching; Heish, Ning Ning; Tseng, Yun Long; Huang, Kuang Liang; Chuang, Kuo Tang; Chen, Chin Hsiung; Hwang, Jeng Jong; Lin, Wuu Jyh; Wang, Shyh Jen; Ting, Gann; Whang-Peng, Jacqueline; Deng, Win Ping.

In: Nuclear Instruments and Methods in Physics Research, Section A: Accelerators, Spectrometers, Detectors and Associated Equipment, Vol. 569, No. 2 SPEC. ISS., 20.12.2006, p. 533-537.

Research output: Contribution to journalArticle

Wang, Hsin Ell ; Yu, Hung Man ; Lu, Yi Ching ; Heish, Ning Ning ; Tseng, Yun Long ; Huang, Kuang Liang ; Chuang, Kuo Tang ; Chen, Chin Hsiung ; Hwang, Jeng Jong ; Lin, Wuu Jyh ; Wang, Shyh Jen ; Ting, Gann ; Whang-Peng, Jacqueline ; Deng, Win Ping. / Internal radiotherapy and dosimetric study for 111In/177Lu-pegylated liposomes conjugates in tumor-bearing mice. In: Nuclear Instruments and Methods in Physics Research, Section A: Accelerators, Spectrometers, Detectors and Associated Equipment. 2006 ; Vol. 569, No. 2 SPEC. ISS. pp. 533-537.
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abstract = "In vivo characterization and dosimetric analysis has been performed to evaluate the potential of pegylated liposomes as carriers of radionuclides in tumor internal radiotherapy. Methods: The DTPA/PEG-liposomes were synthesized with a medium size of 110 nm, conjugated with 111In/177Lu-(oxine)3 to afford 111In/177Lu-liposome. The stability of 111In/177Lu-liposome in serum was investigated. The biodistribution, scintigraphic imaging and pharmacokinetics of 111In/177Lu-liposomes after intravenous(i.v.) injection into C-26 tumor-bearing BALB/cByJ mice were studied. Radiation dose was estimated by MIRD-III program. Results: The incorporation efficiency of 111In/177Lu into liposomes was 95{\%}. After incubation at 37 °C for 72 h in serum, more than 83{\%} of radioactivity was still retained in the intact 111In/177Lu-liposomes. The biodistribution of 111In-liposomes showed that the radioactivity in the blood decreased from 23.14±8.16{\%}ID/g at 1 h to 0.02±0.00{\%}ID/g at 72 h post-injection (p.i.), while reaching its maximum accumulation in tumors at 48 h p.i., with half-life in blood of 10.2 h. The results were supported by that of 177Lu-liposomes. Scintigraphic imaging with 111In-liposomes showed unambiguous tumor images at 48 h p.i. Dose estimation showed that the absorbed dose in tumor from 177Lu-liposomes was 5.74×10-5 Gy/MBq. Conclusions: This study provides an in vivo characterization and dosimetric evaluation for the use of liposome systems as carriers in targeted radionuclide therapy. The results suggest that adequate tumor targeting as well as dose delivered to tumors could be achieved by the use of radionuclide targeted liposomes.",
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AU - Wang, Hsin Ell

AU - Yu, Hung Man

AU - Lu, Yi Ching

AU - Heish, Ning Ning

AU - Tseng, Yun Long

AU - Huang, Kuang Liang

AU - Chuang, Kuo Tang

AU - Chen, Chin Hsiung

AU - Hwang, Jeng Jong

AU - Lin, Wuu Jyh

AU - Wang, Shyh Jen

AU - Ting, Gann

AU - Whang-Peng, Jacqueline

AU - Deng, Win Ping

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N2 - In vivo characterization and dosimetric analysis has been performed to evaluate the potential of pegylated liposomes as carriers of radionuclides in tumor internal radiotherapy. Methods: The DTPA/PEG-liposomes were synthesized with a medium size of 110 nm, conjugated with 111In/177Lu-(oxine)3 to afford 111In/177Lu-liposome. The stability of 111In/177Lu-liposome in serum was investigated. The biodistribution, scintigraphic imaging and pharmacokinetics of 111In/177Lu-liposomes after intravenous(i.v.) injection into C-26 tumor-bearing BALB/cByJ mice were studied. Radiation dose was estimated by MIRD-III program. Results: The incorporation efficiency of 111In/177Lu into liposomes was 95%. After incubation at 37 °C for 72 h in serum, more than 83% of radioactivity was still retained in the intact 111In/177Lu-liposomes. The biodistribution of 111In-liposomes showed that the radioactivity in the blood decreased from 23.14±8.16%ID/g at 1 h to 0.02±0.00%ID/g at 72 h post-injection (p.i.), while reaching its maximum accumulation in tumors at 48 h p.i., with half-life in blood of 10.2 h. The results were supported by that of 177Lu-liposomes. Scintigraphic imaging with 111In-liposomes showed unambiguous tumor images at 48 h p.i. Dose estimation showed that the absorbed dose in tumor from 177Lu-liposomes was 5.74×10-5 Gy/MBq. Conclusions: This study provides an in vivo characterization and dosimetric evaluation for the use of liposome systems as carriers in targeted radionuclide therapy. The results suggest that adequate tumor targeting as well as dose delivered to tumors could be achieved by the use of radionuclide targeted liposomes.

AB - In vivo characterization and dosimetric analysis has been performed to evaluate the potential of pegylated liposomes as carriers of radionuclides in tumor internal radiotherapy. Methods: The DTPA/PEG-liposomes were synthesized with a medium size of 110 nm, conjugated with 111In/177Lu-(oxine)3 to afford 111In/177Lu-liposome. The stability of 111In/177Lu-liposome in serum was investigated. The biodistribution, scintigraphic imaging and pharmacokinetics of 111In/177Lu-liposomes after intravenous(i.v.) injection into C-26 tumor-bearing BALB/cByJ mice were studied. Radiation dose was estimated by MIRD-III program. Results: The incorporation efficiency of 111In/177Lu into liposomes was 95%. After incubation at 37 °C for 72 h in serum, more than 83% of radioactivity was still retained in the intact 111In/177Lu-liposomes. The biodistribution of 111In-liposomes showed that the radioactivity in the blood decreased from 23.14±8.16%ID/g at 1 h to 0.02±0.00%ID/g at 72 h post-injection (p.i.), while reaching its maximum accumulation in tumors at 48 h p.i., with half-life in blood of 10.2 h. The results were supported by that of 177Lu-liposomes. Scintigraphic imaging with 111In-liposomes showed unambiguous tumor images at 48 h p.i. Dose estimation showed that the absorbed dose in tumor from 177Lu-liposomes was 5.74×10-5 Gy/MBq. Conclusions: This study provides an in vivo characterization and dosimetric evaluation for the use of liposome systems as carriers in targeted radionuclide therapy. The results suggest that adequate tumor targeting as well as dose delivered to tumors could be achieved by the use of radionuclide targeted liposomes.

KW - Dosimetry

KW - Indium-111

KW - Lutetium-177

KW - Radiolabeled pegylated liposomes

KW - Targeted radionuclide therapy

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