• Bulletin of the Korean Chemical Society
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• v.33 no.2
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• pp.489-491
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• 2012

An $^{125}I$-labeled resveratrol derivative 1 was synthesized. It was purified by reverse phase HPLC. Radiochemical purity of the product was more than 98%, and the yield was 35% (decay-corrected). Its biodistribution in tumorbearing mice was studied. The results showed that the highest radioactivity was located in intestine and stomach. The biodistribution profile suggests that compound 1 can be effectively used as a promising imaging probe for intestine and stomach.

• Journal of Radiation Industry
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• v.12 no.4
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• pp.355-363
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• 2018

A novel $N_3S_1$ chelate, Pro-Lys-Cys (PKC) to cyclic RGD to radiolabel with $^{99m}Tc$ was conjugated in an effort to decrease the high intestinal accumulation observed for $^{99m}Tc$-labeled PGC-RGD. The target specificity of the resulting PKC-RGD was similar to that of PGC-RGD as determined by a cell binding assay and a competition binding assay. The $^{99m}Tc$ radiolabeling of PKC-RGD resulted in radiochemical yields of 98% under mild conditions at high specific activities. Biodistribution data in normal mice clearly showed a significant decrease in intestinal uptake at 2 h postinjection for the $^{99m}Tc-PKC-c$ (RGDyK) compared to the $^{99m}Tc-GC-c$ (RGDyK) (from $19.65%ID{\cdot}g^{-1}$ to $7.31%ID{\cdot}g^{-1}$ for the GI tract). The $^{99m}Tc-PKC-c$ (RGDyK) biodistribution was also shown by a higher retention of radioactivity in the whole body, but with kidney accumulation over 8-fold higher than observed with $^{99m}Tc-PGC-c$ (RGDyK) at 2 h ($12.62%ID{\cdot}g^{-1}$ for PKC-RGD and $1.54%ID{\cdot}g^{-1}$ for PGC-RGD, respectively). These results show that the biodistribution may be altered especially concerning lipophilicity resulting in renal rather than hepatobiliary excretion. This comparative study made it possible to explore the effects of lipophilicity on the biodistribution of $^{99m}Tc$-labeled c (RGDyK) through the use of different tripeptide $N_3S_1$ chelators. Therefore, $^{99m}Tc-PKC-c$ (RGDyK) may be an attractive alternative for the in vivo imaging of integrin receptors.

• Advances in nano research
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• v.10 no.5
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• pp.461-470
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• 2021

Infection is one of the major mortality causes throughout the globe. Nuclear medicine plays an important role in diagnosis of deep infections such as osteomyelitis, arthritis infection, heart valve and heart prosthesis infections. Techniques such as labeled leukocytes are sensitive and selective for tracking the inflammations but they are not suitable for differentiating infection from inflammation. Anionic linear-globular dendrimer-G₂ was synthesized then conjugation to gemifloxacin antibiotic. The structures were identified by FT-IR, ¹H-NMR, C-NMR, LC-MS and DLS. The toxicity of gemifloxacin and dendrimer-gemifloxacin complex was compared by MTT test. Dendrimer-G₂-gemifloxacin was labeled by Technetium-99m and its in-vitro stability and radiochemical purity were investigated. In-vivo biodistribution and SPECT imaging were studied in a rabbit model. Identify and verify the structure of the each object was confirmed by FT-IR, ¹H-NMR, C-NMR and LC-MS, also, the size and charge of this compound were 128 nm and -3/68 mv respectively. MTT test showed less toxicity of the dendrimer-G₂-gemifloxacin than free gemifluxacin (P < 0.001). Radiochemical yield was > %98. Human serum stability was 84% up to 24 h. Biodistribution study at 50 min, 24 and 48 h showed that the complex is significantly absorbed by the intestine and accumulation in the lungs and affects them, finally excreted through the kidneys, biodistribution results are consistent with results from full image means of SPECT/CT technique.

• Nuclear Engineering and Technology
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• v.55 no.1
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• pp.295-303
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• 2023

Whole-body counters are widely used to assess internal contamination after a nuclear accident. However, it is difficult to determine radioiodine activity due to limitations in conventional calibration phantoms. Inhaled or ingested radioiodine is heterogeneously distributed in the human body, necessitating time-dependent biodistribution for the assessment of the internal contamination caused by the radioiodine intake. This study aims at calculating counting efficiencies considering the biodistribution of ¹³¹I in whole-body counting measurement. Monte Carlo simulations with computational human phantoms were performed to calculate the whole-body counting efficiency for a realistic radioiodine distribution after its intake. The biodistributions of ¹³¹I for different age groups were computed based on biokinetic models and applied to age- and gender-specific computational phantoms to estimate counting efficiency. After calculating the whole-body counting efficiencies, the efficiency correction factors were derived as the ratio of the counting efficiencies obtained by considering a heterogeneous biodistribution of ¹³¹I over time to those obtained using the BOMAB phantom assuming a homogeneous distribution. Based on the correction factors, the internal contamination caused by ¹³¹I can be assessed using whole-body counters. These correction factors can minimize the influence of the biodistribution of ¹³¹I in whole-body counting measurement and improve the accuracy of internal dose assessment.

• The Korea Journal of Herbology
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• v.22 no.2
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• pp.181-188
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• 2007

Objectives : This study was to verify the Attributive Channel theory of herbal medicine. Methods : [13lI]iodocurcumin was synthesized, separated, and refined from curcumin, the major component of Curcuma species, followed by observing the biodistribution in an organism. Especially, from the fact that curcumin has shown to possess potent anti-carcinogenic properties, the biodistribution in the carcinogenesis organism was analyzed. Result : Iodocurcumin 23mg was obtained through column chromatography after a reaction with 50mg of Curcumin and ICl. The nominal yield of [13lI]iodocurcumin synthesis was 35% when checked with radioactive layer of chromatography. [13lI]iodocurcumin was most largely distributed in the stomach of a BALB/c mouse and a C57BL/6 mouse transplanted with Lewis lung carcinoma cell. Conclusion : The fact that [13lI]iodocurcumin was most largely distributed in the stomach was related with the Attributive Channel theory. And there was no significant finding related to tumor cells.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.71-77
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• 2001

We recently developed a high efficiency expression vectors pCK, which drives a high level of gene expression in the skeletal muscles of mice. In this study, we investigated the pharmacokinetics and biodistribution of pCK-VEGF expressing human VEGF165 after intravenous or intramuscular administration. The quantity of pCK-VEGF in the tissues of mice was measured by the PCR method which has a detection limit of approximately 1 pg of the exogenously added plasmid. In the case of intravenous administration, the half life of the pCK-VEGF plasmid in the bloodstream was 1.68 min. After intra-muscular administration, the half life of pCK-VEGF plasmid in the bloodstream was 6.78 min. At 90 min post-administration, 30% of the injected pCK-VEGF was found at the site of injection, where it persisted for up to 8 hours. Less than 1.6% of the injected pCK-VEGF plasmid DNA was detected in highly vascularized tissues such as the lung, kidney; and liver at 90 min post-administration, but the plasmid was undetectable at later time points. These results suggested that intramuscularly administrated pCK-VEGF persisted for longer periods of time in muscles than in other tissues and that direct intra-muscular injection of pCK-VEGF might be useful for local therapeutic angiogenesis.

• Investigative Magnetic Resonance Imaging
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• v.23 no.1
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• pp.34-37
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• 2019

Gadolinium contrast agents (CAs) are integral components of clinical magnetic resonance imaging (MRI). However, safety concerns have arisen regarding the use of gadolinium CAs, due to their association with nephrogenic systemic fibrosis (NSF). Furthermore, recently the long-term retention of $Gd^{3+}-based$ CAs in brains patients with normal renal function raised another possible safety issue. The safety concerns of $Gd^{3+}-based$ CAs have been based on the ligand structure of $Gd^{3+}-based$ CAs, and findings that $Gd^{3+}-based$ CAs with linear ligand structures showed much higher incidences of NSF and brain retention of CAs than $Gd^{3+}-based$ CAs with macrocyclic ligand structure. In the current study, we report the in vivo biodistribution profile of a new highly stable multifunctional $Gd^{3+}-based$ CA, with macrocyclic ligand structure (HNP-2006). MR imaging using HNP-2006 demonstrated a significant contrast enhancement in many different organs. Furthermore, the contrast enhanced tumor imaging using HNP-2006 confirmed that this new macrocyclic CA can be used for detecting tumor in the central nervous system. Therefore, this new multifunctional HNP-2006 with macrocyclic ligand structure shows great promise for whole-body clinical application.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.626-635
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• 2005

Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistr ibution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied. Compared with the 'fluid' liposome (S-Lip) composed of soybean phosphatidylcholine (SPC), the 'solid' liposome (H-Lip) composed of hydrogenated soybean phosphatidylcholine HSPC decreased the leaking efficiency of TPT from liposome and enhanced the stability of liposome in fetal bovine serum (FBS) or human blood plasma (HBP). The results of biodistribution studies in S$_{180}$ tumor-bearing mice showed that liposomal encapsulation increased the concentrations of total TPT and the ratio of lactone form in plasma. Compared with free TPT, S-Lip and H-Lip resulted in 5- and 19- fold increase in the area under the curve (AUC$_{0\rightarrow\propto}$), respectively. PEG- modified H-Lip (H-PEG) showed 3.7-fold increase in AUC$_{0\rightarrow\propto}$ compared with H-Lip, but there was no significant increase in t$_{1/2}$ and AUC$_{0\rightarrow\propto}$ for PEG-modified S-Lip (S-PEG) compared with S-Lip. Moreover, the liposomal encapsulation changed the biodistribution behavior, and H-Lip and H-PEG dramatically increased the accumulation of TPT in tumor, and the relative tumor uptake ratios were 3.4 and 4.3 compared with free drug, respectively. There was also a marked increase in the distribution of TPT in lung when the drug was encapsulated into H-Lip and H-PEG. Moreover, H-PEG decreased the accumulation of TPT in bore marrow compared with unmodified H-Lip. All these results indicated that the membrane fluidity of liposome has an important effect on in vitro stability and in vivo biodistribution pattern of liposomes containing TPT, and PEG-modified 'solid' liposome may be an efficient carrier of TPT.

• Macromolecular Research
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• v.11 no.1
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• pp.19-24
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• 2003

Polymeric gene delivery system attracts profound attention as it shows less toxicity, versatility, and reasonable gene expression efficiency. Terplex system, a synthetic biopolymeric gene delivery system consisting of stearyl poly-L-lysine (stearyl-PLL) and low density lipoprotein (LDL) was evaluated for its body distribution of gene expression of exogenously administered pDNA after tail-vein injection in mice. Kidney and spleen are two major organs with highest gene expression, whereas liver and heart showed marginal gene expression among the organs examined. Hemolytic effect of the terplex system was evaluated using human red blood cells, where terplex system did not cause significant hemolysis at the concentrations above the experimental ranges, although unmodified PLL or stearyl-PLL without LDL did. Serum stability of terplex system against enzymatic degradation was also significantly enhanced, presumably due to the steric stabilization from the polymers. Based on these findings and along with its high in vitro transfection efficiency, terplex system could serve as a safe and efficient polymeric gene delivery system with many applications for the in vivo gene therapy.

• 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.