• Title/Summary/Keyword: Biodistribution

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177Lu-EDTMP radiation absorbed dose evaluation in man based on biodistribution data in Wistar rats

  • Reza Bagheri
    • Nuclear Engineering and Technology
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    • v.55 no.1
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    • pp.254-260
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    • 2023
  • Skeletal metastases are common in patients suffering from various primary cancers. Radiopharmaceuticals are an effective option for bone pain palliation. In this work, the radiation absorbed dose of 177Lu-EDTMP radiopharmaceutical was estimated for adult man based on biodistribution data in Wistar rats. The MIRD dose calculation method and the Sparks and Aydogan methodology were applied. The results shows that about 46% of injected activity is cumulated on the surface of the trabecular and cortical bones. Radiation absorbed doses of red bone marrow and osteogenic cells were estimated to about 1.1 and 6.2 mGy/MBq, respectively. The maximum administrated activity was obtained 27 MBq/kg of body weight with an effective dose of 0.23 mSv/MBq. The results were compared with other available data from literature. This study indicated that 177Lu-EDTMP provides therapeutic efficacy for achieving bone pain palliation with low undesired dose to other normal organs.

Characteristics of HIV-Tat Protein Transduction Domain

  • Yoon Jong-Sub;Jung Yong-Tae;Hong Seong-Karp;Kim Sun-Hwa;Shin Min-Chul;Lee Dong-Gun;Shin Wan-Shik;Min Woo-Sung;Paik Soon-Young
    • Journal of Microbiology
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    • v.42 no.4
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    • pp.328-335
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    • 2004
  • The human immunodeficiency virus type 1 (HIV-I) Tat protein transduction domain (PTD), which con­tains rich arginine and lysine residues, is responsible for the highly efficient transduction of protein through the plasma membrane. In addition, it can be secreted from infected cells and has the ability to enter neighboring cells. When the PTD of Tat is fused to proteins and exogenously added to cells, the fusion protein can cross plasma membranes. Recent reports indicate that the endogenously expressed Tat fusion protein can demonstrate biodistribution of several proteins. However, intercellular transport and protein transduction have not been observed in some studies. Therefore, this study exam­ined the intercellular transport and protein transduction of the Tat protein. The results showed no evi­dence of intercellular transport (biodistribution) in a cell culture. Instead, the Tat fusion peptides were found to have a significant effect on the transduction and intercellular localization properties. This sug­gests that the HIV-1 PTD passes through the plasma membrane in one direction.

Altered Biodistribution of Gallium-67 in a Patient with Multiple Factors Influencing Iron-transport Protein Saturation (철운반단백질 포화정도에 따른 Gallium-67 체내분포의 변화: 증례보고)

  • Choi, Joon Young;Kim, Sang Eun;Lee, Kyung Han;Kim, Byung-Tae
    • The Korean Journal of Nuclear Medicine
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    • v.32 no.1
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    • pp.114-119
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    • 1998
  • We present a case of a young female patient with fulminant hepatitis who showed an altered biodistribution of Ga-67, after being scanned twice at 10 month intervals. On initial scan, uplake of Ga-67 was increased in the liver, kidneys, and skeletons. Increased hepatic Ga-67 uptake may be explained by increased transferrin unbound Ga-67 that was taken up by the inflamed liver. The saturation of iron-binding proteins due to multiple transfusions may lead to increased renal and skeletal Ga-67 uptake. On follow-up scan hepatic Ga-67 uptake was markedly increased. Also increased Ga-67 uptake in the axial skeleton and normalized renal uptake were shown. The findings were consistent with iron deficiency anemia. This case demonstrates altered Ga-67 biodistribution associated with multiple transfusions, fulminant hepatitis, and iron deficiency anemia.

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Synthesis and $^{18}F$ Labelling of Organic Ammonium Salts to New Cardiac Flow Tracer for PET and Their Biodistribution (양전자단층촬영에 이용 가능한 새로운 심근 혈류 추적자 개발; F-18이 표지된 유기암모늄염의 합성과 체내분포에 관한 연구)

  • Yu, Kook-Hyun
    • The Korean Journal of Nuclear Medicine
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    • v.28 no.3
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    • pp.331-337
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    • 1994
  • In order to develop a $^{18}F$-labelled myocardial perfusion agent(flow tracer) for PET, $^{18}F$-labelled organic ammonium cations were synthesized and evaluated in relation to their biodistribution. Five quaternary organic ammonium compounds were labelled with $^{18}F$ in a side chain with moderate to good yields by direct introduction of $^{18}F$-fluoride. Radiochemical yields have been achieved in 30-40min by the precursors (tosylates) in dimethylsulfoxide 15-60% (decay corrected). The reaction was found to be autocatalyzed. A remote controlled procedure was developed in these synthesis. $^{18}F$-Labelling and HPLC-purification of com-pounds needed about 60 min(Yield; 7-20%). Up to now the two compounds N-4-[$^{18}F$]fluorobutyl-pyridinium cation(1) and N, N dibenzyl-4(2-[$^{18}F$]fluoroethyl)piperidinium cation(2) were investigated in relation to their biodistribution in mice. Compound 1 showed at 1 min post injection the high uptake of 19.22% ID/g organ in the myocardium but a following fast decline to 1.12% ID/g organ after 40min. Uptake of compound 2 was after 1min in the heart 5.90% ID/g organ but after 40min at the relative high value of 4.33% ID/g organ. Heart:blood ratio for compound(1) at 1 min was 8.3, at 40 min 2.6 for compound II 2.0(1min) and 15.0(40 min). As data of compound 2 showed greater heart uptake, slower myocardial release, and higher heart: blood ratios, compound 2 is a good candidate for further evaluation.

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Pharmacokinetic Behavior and Biodistribution of Paclitaxel-Loaded Lipid Nanosuspension

  • Choi, Sung-Up;Park, Jung-Min;Choi, Woo-Sik;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.39 no.5
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    • pp.359-366
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    • 2009
  • In this study, paclitaxel-loaded lipid nanosuspension (PxLN) was prepared and the in vivo profiles after intravenous administration in rats were investigated. We compared the manufacturing processes depending on the temperature: PxLN-H for a hot homogenization process and PxLN-C for solidification of lipid-drug mixtures by liquid nitrogen. Both formulations showed submicron size distribution and the similar drug loading efficiency of about 70%. In vitro release of PxLNs and Taxol$^{(R)}$ performed by a dialysis diffusion method showed similar pattern for PxLN-H and Taxol$^{(R)}$, but the reduced release profile for PxLN-C. PxLN or Taxol$^{(R)}$ was intravenously administered to the rats at a dose of 5 mg/kg as paclitaxel. The drug in blood samples were assayed by the HPLC/MS/MS method. The AUC$_t$ of PxLN-H was 3.4-fold greater than that of Taxol$^{(R)}$. PxLN-H gave higher biodistribution in all tissues than did Taxol$^{(R)}$. In addition, it maintained the higher drug concentration for 12 h. This lipid nanosuspension might be a promising candidate for an alternative formulation for the parenteral delivery of poorly water-soluble paclitaxel.

Synthesis and biodistribution of 18F-labeled α-, β- and ω-fluorohexadecanoic acid

  • Lee, Yun-Sang;Kim, Young Joo;Cheon, Gi Jeong;Jeong, Jae Min
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.4 no.2
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    • pp.57-64
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    • 2018
  • ${\omega}-[^{18}F]$-Fluorohexadecanoic acid (FHA) has been used for imaging of fatty acid metabolism of myocardium. To increase retention of radiolabeled fatty acid by blocking ${\beta}$-oxidation, methyl branched analogues have been used. In this experiment, we tried to synthesize 18F-labeled ${\alpha}-$, ${\beta}-$ and ${\omega}-FHA$ for imaging of the myocardial fatty acid metabolism. We synthesized ${\alpha}-$, ${\beta}-$ and ${\omega}$-mesylated methyl hexadecanoates and labeled with $^{18}F$ by reacting with $[^{18}F]$TBAF in acetonitrile at $80^{\circ}C$ for 10 min. Methyl ester group was removed by 1 M NaOH at $80^{\circ}C$ for 5 min. The yields of ${\alpha}-[^{18}F]$ and ${\omega}-[^{18}F]FHA$ were 25.5 and 45.5%, respectively [EOS]. However, ${\beta}-[^{18}F]FHA$ was not labeled at all due to a fast elimination reaction. The biodistribution study in ICR-mice showed that ${\omega}-[^{18}F]FHA$ has higher myocardial uptake and lower liver uptake than ${\alpha}-[^{18}F]FHA$. The electron-withdrawing effect of fluorine at ${\alpha}-$ position is believed to be the major factor affecting the biodistribution.