Preparation and in vivo biological investigations on a novel radioligand for bone scanning: technetium-99m-labeled zoledronic acid derivative

Lin, Jianguo; Qiu, Ling; Cheng, Weiguo; Luo, Songyuan; Ye, Wanzhong

doi:10.1016/j.nucmedbio.2010.12.005

Cited by 26 publications

(14 citation statements)

References 18 publications

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“…Bisphosphonate compounds are strong chelating agents, the reaction of bisphosphonate compounds with technetium gave only three species (free pertechnetate 99m TCO 4 − , colloid, and 99m Tc‐complex) where the structure of the complex is formed from two molecules of bisphosphonate and one technetium atom like all previously reported bisphosphonates as shown in Figure .…”

Section: Methodssupporting

confidence: 59%

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

Motaleb

Adli

El-Tawoosy

et al. 2016

J. Label Compd. Radiopharm

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This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2 .2H2 O and NaBH4 ) where NaBH4 gave stable complex and higher radiochemical yield more than SnCl2 .2H2 O. The results showed that, the radiochemical purity of (99m) Tc(NaBH4 )-risedronate was 99.2 ± 0.6% and its stability was up to 6 h. Biodistribution study showed high uptake and long retention of (99m) Tc(NaBH4 )-risedronate in bone starting from 15 min (29 ± 2.5% ID/organ) up to 4 h (35.1 ± 3.2 ID/organ) post injection. This research could introduce an easy and effective method for synthesis and labeling of risedrionate and affording a good tracer for bone imaging.

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Section: Methodssupporting

confidence: 59%

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

Motaleb

Adli

El-Tawoosy

et al. 2016

J. Label Compd. Radiopharm

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“…This may reflect the higher uptake of PEG‐ALE by macrophages when delivered in a nanoparticulate form. Because of their high hydrophilicity (logP from ‐1 to ‐5),63, 64 bisphosphonates exhibit poor membrane permeability. These results are in line with those of Salzano et al , who observed an increased in vitro activity of bisphosphonate delivered in particles, compared to free bisphosphonate 65.…”

Section: Resultsmentioning

confidence: 99%

siRNA Transfection with Calcium Phosphate Nanoparticles Stabilized with PEGylated Chelators

Giger¹,

Castagner²,

Räikkönen³

et al. 2012

Adv Healthcare Materials

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Despite the enormous therapeutic potential of siRNAs, their delivery is still problematic due to unfavorable biodistribution profiles and poor intracellular bioavailability. Calcium phosphate co-precipitate has been used for nearly 40 years for in vitro transfection due to its non-toxic nature and simplicity of preparation. However, rapid particle growth has largely prevented the translation of this method for in vivo purposes. It has recently been shown that bisphosphonate derivatives can physically stabilize calcium phosphate nanoparticles while still allowing for efficient cell transfection with plasmid DNA. Herein, two novel PEGylated chelating agents (PEG-alendronate and PEG-inositolpentakisphosphate) with enhanced stabilizing properties are introduced, and it is demonstrated that the bisphosphonate-stabilized nanoparticles can efficiently deliver siRNA in vitro. The nanoparticles are mainly taken up by clathrin-dependent endocytosis, and acidification of the endosomal compartment is required to release the entrapped siRNA into the cytosol. Furthermore, particle uptake enhances the inhibition of the mevalonate pathway by the bisphosphonate in macrophages.

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“…According to literature, [32] the binding rate to HSA affects the blood clearance of the radiolabeled complex. According to literature, [32] the binding rate to HSA affects the blood clearance of the radiolabeled complex.…”

Section: Hsa Binding and Hydroxyapatitebinding Assaymentioning

confidence: 99%

Synthesis and evaluation of a novel ^99mTc nitrido radiopharmaceutical with alendronate dithiocarbamate as a potential bone‐imaging agent

et al. 2017

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Currently, a popular strategy for designing novel radioprobes as bone-imaging agents is based on the concept of bifunctional radiopharmaceuticals. Considering the dithiocarbamate ligand can act as a suitable bifunctional linking agent to attach technetium-99m ( Tc) to corresponding target molecules, in this study, alendronate dithiocarbamate (ALNDTC) was synthesized and radiolabeled with [ Tc≡N] core by ligand exchange reaction to produce TcN-ALNDTC complex, for the potential use as a novel probe for bone imaging. The radiochemical purity of the complex was over 90%. The complex was stable in vitro and could bind to hydroxyapatite. The partition coefficient result indicated it was hydrophilic, and an evaluation of biodistribution in mice indicated that the complex exhibited a higher bone uptake than did Tc-labeled methylenediphosphonate ( Tc-MDP). Further, single photon emission computed tomography imaging study indicated clear accumulation in bone, suggesting that TcN-ALNDTC would be a promising candidate for bone imaging.

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Preparation and in vivo biological investigations on a novel radioligand for bone scanning: technetium-99m-labeled zoledronic acid derivative

Cited by 26 publications

References 18 publications

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

siRNA Transfection with Calcium Phosphate Nanoparticles Stabilized with PEGylated Chelators

Synthesis and evaluation of a novel ^99mTc nitrido radiopharmaceutical with alendronate dithiocarbamate as a potential bone‐imaging agent

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Preparation and in vivo biological investigations on a novel radioligand for bone scanning: technetium-99m-labeled zoledronic acid derivative

Cited by 26 publications

References 18 publications

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

siRNA Transfection with Calcium Phosphate Nanoparticles Stabilized with PEGylated Chelators

Synthesis and evaluation of a novel 99mTc nitrido radiopharmaceutical with alendronate dithiocarbamate as a potential bone‐imaging agent

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Synthesis and evaluation of a novel ^99mTc nitrido radiopharmaceutical with alendronate dithiocarbamate as a potential bone‐imaging agent