Preparation and biological profile of 99mTc-lidocaine as a cardioselective imaging agent using 99mTc eluted from 99Mo/99mTc generator based on Al–Mo gel

Sakr, Tamer M.; Ibrahim, A. B.; Fasih, T. W.; Rashed, Hassan M.

doi:10.1007/s10967-017-5560-z

Cited by 18 publications

(15 citation statements)

References 38 publications

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“…Direct labeling technique was used for radiolabeling of the optimized CLZ-loaded PNMS formula with technetium-99 ( 99m Tc) as a tracer (Ibrahim et al, 2014 ; Nour et al, 2016 ; Sakr et al, 2017 ). Sodium dithionite (Na 2 S 2 O 4 ) has been used as a reducing agent for direct radiolabeling of the optimum formula with 99m Tc ( t 1/2 =6 h) to skip the interference of colloidal stannic oxide with the biodistribution results, when the most familiar reducing agent (stannous chloride) is used (Qi et al, 1996 ; Geskovski et al, 2013 ).…”

Section: Methodsmentioning

confidence: 99%

“…By using a NaI (Tl) γ-ray scintillation counter, each radioactivity for tissue/organ/fluid in addition to the background radioactivity was computed. Muscles, bone, and blood were assumed to be 40, 10, and 7% of the total body mass, respectively, to detect their weigh (Motaleb et al, 2011 ), % ID/g which is the % of the injected dose per gram (fluid, tissue, or organ) at the prearranged time points in a group consisting of three mice were computed through the following equation (Sakr et al, 2017 ): …”

Section: Methodsmentioning

confidence: 99%

“…Radiolabelling using 99m Tc. Direct labeling technique was used for radiolabeling of the optimized CLZloaded PNMS formula with technetium-99 ( 99m Tc) as a tracer(Ibrahim et al, 2014;Nour et al, 2016;Sakr et al, 2017).…”

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confidence: 99%

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Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

Sayed

Elsharkawy²,

Amin

et al. 2021

Drug Delivery

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The research objective is to design intranasal (IN) brain targeted CLZ-loaded polymeric nanomicellar systems (PNMS) aiming to improve central systemic CLZ bioavailability. Direct equilibrium method was used to prepare CLZ-PNMS using two hydrophobic poloxamines; Tetronic V R 904 (T904) and Tetronic V R 701 (T701) and one hydrophilic poloxamer; Synperonic V R PE/F127 (F127). Optimization is based on higher percent transmittance, solubilizing efficiency, and in vitro release after 24 h with smaller particle size was achieved using Design-Expert V R software. The optimized formula was further evaluated via TEM, ex vivo nasal permeation in addition to in vivo biodistribution using radiolabeling technique of the optimized formula by Technetium-99m ( 99m Tc). The optimized formula M5 has small size (217 nm) with relative high percentage of transmittance (97.72%) and high solubilization efficacy of 60.15-fold following 92.79% of CLZ released after 24 h. Ex vivo nasal permeation showed higher flux of 36.62 lg/ cm 2 .h compared to 7.324 lg/cm 2 .h for CLZ suspension with no histological irritation. In vivo biodistribution results showed higher values of radioactivity percentage of the labeled optimized formula ( 99m Tc-M5) in brain and brain/blood ratio following IN administration of 99m Tc-M5 complex which were greater than their corresponding values following intravenous route. It is obvious that nasal delivery of CLZ-PNMS could be a promising way to improve central systemic CLZ bioavailability.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

Sayed

Elsharkawy²,

Amin

et al. 2021

Drug Delivery

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“…Dual solvent systems were used as mobile phases to determine the labeling yield. Acetone was used to determine the free 99m TcO 4 − percentage where its R f is 0.95 while 99m Tc-phosphinothricin and 99m Tc-colloidal remain in the origin, while ethanol:water:ammonium hydroxide mixture (2:5:1, v / v / v ) was used to determine the 99m Tc-colloidal impurities where its R f is 0 while 99m Tc-phosphinothricin and 99m TcO 4 − move to the front [ 29 , 30 , 31 ].…”

Section: Methodsmentioning

confidence: 99%

In Silico-Based Repositioning of Phosphinothricin as a Novel Technetium-99m Imaging Probe with Potential Anti-Cancer Activity

et al. 2018

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l-Phosphinothricin (glufosinate or 2-amino-4-((hydroxy(methyl) phosphinyl) butyric acid ammonium salt (AHPB)), which is a structural analog of glutamate, is a recognized herbicide that acts on weeds through inhibition of glutamine synthetase. Due to the structural similarity between phosphinothricin and some bisphosphonates (BPs), this study focuses on investigating the possibility of repurposing phosphinothricin as a bisphosphonate analogue, particularly in two medicine-related activities: image probing and as an anti-cancer drug. As BP is a competitive inhibitor of human farnesyl pyrophosphate synthase (HFPPS), in silico molecular docking and dynamic simulations studies were established to evaluate the binding and stability of phosphinothricin with HFPPS, while the results showed good binding and stability in the active site of the enzyme in relation to alendronate. For the purpose of inspecting bone-tissue accumulation of phosphinothricin, a technetium (99mTc)–phosphinothricin complex was developed and its stability and tissue distribution were scrutinized. The radioactive complex showed rapid, high and sustained uptake into bone tissues. Finally, the cytotoxic activity of phosphinothricin was tested against breast and lung cancer cells, with the results indicating cytotoxic activity in relation to alendronate. All the above results provide support for the use of phosphinothricin as a potential anti-cancer drug and of its technetium complex as an imaging probe.

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“…Gold nanoparticulates functionalized with doxorubicin would also present attractive prospects for labeling with Single Photon Emitting Computed Tomographic (SPECT) radioisotopes such as 99m Tc. 99m Tc radiopharmaceuticals provide excellent SPECT images of tumors/lesions [39][40][41]. Therefore, multiplexing of doxorubicin-loaded gold nanoparticles and subsequent labeling of such therapeutic conjugates with 99m Tc opens up new avenues in the design and development of theranostic agents with applications in oncology [42][43][44][45][46].…”

Section: Introductionmentioning

confidence: 99%

Preparation, Characterization, Cytotoxicity and Biological Evaluation of <sup>99m</sup>Tc-Doxorubicin-Epigallocatechingallate Functionalized Gold Nanoparticles as a New Generation of Theranostic Radiopharmaceutical

Sakr¹,

Morsy²,

Na³

et al. 2018

Preprint

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Gold nanoparticles are currently used for the treatment of cancer through a myriad of modalities and delivery approaches. Conjugation of tumor imaging Single Photon Emitting Computed Tomographic (SPECT) radiopharmaceutical to gold nanoparticles will allow systemic targeting and imaging of cancer tissues simultaneously. In this study, gold nanoparticles (AuNPs) were prepared using Epigallocatechingallate (EGCG), loaded with doxorubicin (Dox), and characterized before and after doxorubicin conjugation. Cytotoxicity of EGCG-AuNPs and Dox-EGCG-AuNPs were evaluated against breast carcinoma (MCF-7) and hepatocellular carcinoma (HepG-2) cell lines demonstrating high cytotoxic effects of Dox-EGCG-AuNPs against both cell lines. Doxorubicin was radiolabeled with 99mTc and our new approach has optimized various labeling conditions resulting in a radiochemical yield of 93.5 ± 2.04%. Biodistribution of 99mTc-Dox-EGCG-AuNPs was studied in normal and tumor bearing mice following I.V. and intratumoral injections at different time intervals. Results showed high uptake of the intravenously injected 99mTc-Dox-EGCG-AuNPs in tumor tissue (22.45 %ID/g at 2 h). In addition, localized intratumoral injection of 99mTc-Dox-EGCG-AuNPs showed extremely high levels of uptake in tumor (80.22 %ID/g at 15 min) with high retention for extended periods post injection. Our results present prospects for the utility of 99mTc-Dox-EGCG-AuNPs as a multiplexed theranostic agent through SPECT imaging of tumor tissue and therapy through photothermal destruction of cancer tissue through the application of exogenous laser lights as well as through tyrosine phosphatases inhibitor (through EGCG), and topoisomerase II inhibitor (through doxorubicin) effects.

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Preparation and biological profile of 99mTc-lidocaine as a cardioselective imaging agent using 99mTc eluted from 99Mo/99mTc generator based on Al–Mo gel

Cited by 18 publications

References 38 publications

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m

In Silico-Based Repositioning of Phosphinothricin as a Novel Technetium-99m Imaging Probe with Potential Anti-Cancer Activity

Preparation, Characterization, Cytotoxicity and Biological Evaluation of <sup>99m</sup>Tc-Doxorubicin-Epigallocatechingallate Functionalized Gold Nanoparticles as a New Generation of Theranostic Radiopharmaceutical

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