Radioiodinated doxorubicin as a new tumor imaging model: preparation, biological evaluation, docking and molecular dynamics

Ibrahim, A. B.; Salem, M. Alaraby; Fasih, T. W.; Brown, Alex; Sakr, Tamer M.

doi:10.1007/s10967-018-6013-z

Cited by 20 publications

(10 citation statements)

References 57 publications

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“…On each paper strip (1 cm × 13 cm), 1-2 μL of the prepared RIRB was seeded 2 cm above the lower edge, evaporated and developed. RIRB developed to R f value of 0.85 while, the free radioiodide (I − ) remained at the spotting point (R f = 0-0.1), after full development, each strip was dried and cut into strips (1 cm) then counted in a well type A NaI (Tl) γ-ray scintillation counter (Scaler Ratemeter SR7, Nuclear Enterprises, Edinburgh, England) [35][36][37].…”

Section: Preparation Of Radioiodinated Rose Bengal Indicatormentioning

confidence: 99%

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator

et al. 2020

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Purpose Adefovir dipivoxil (AD), a nucleoside reverse transcriptase inhibitor is effective against Hepatitis B virus. Its poor oral bioavailability leads to frequent administration causing severe adverse effects. Thereby the entrapment of AD within lipid nanoparticulate systems is a way of increasing AD oral bioavailability as a result of improving intestinal permeability with efficient liver-targeted delivery together with higher drug stability during storage. Methods AD-loaded nanostructured lipid carriers (AD-NLCs) were prepared via solvent emulsification diffusion technique adopting 2 4 full factorial design to study the effect of lipid percentage, presence of egg yolk lecithin, surfactant type and percentage on entrapment efficiency (E.E.%), particle size and percent in-vitro drug released after 8 h (Q8hrs). Results Formula (F12) showed E.E.% of 90.5 ± 0.2%, vesicle size of 240.2 ± 2.5 nm and Q8hrs of 58.55 ± 9.4% was selected as the optimum formula with desirability value of 0.757 based on highest EE%, lowest P.S. and Q8hrs. Further evaluation of the optimized formula using radioiodinated rose bengal (RIRB) in thioacetamide induced liver damage in Swiss Albino mice revealed a higher liver uptake of 22 ± 0.01% ID/g (percent injected dose/g organ) and liver uptake/Blood (T/B) ratio of 2.22 ± 0.067 post 2 h of I.V injection of RIRB compared to 9 ± 0.01% ID/g and 0.64 ± 0.017 in untreated group, respectively. Conclusion NLCs could be successfully used as oral drug delivery carriers of the antiviral drug Adefovir Dipivoxil to the liver with higher stability and oral bioavailability.

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Section: Preparation Of Radioiodinated Rose Bengal Indicatormentioning

confidence: 99%

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator

et al. 2020

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“…Tumor: normal tissue ratio is used as a parameter to evaluate preferential uptake and tumor targeting of a radiolabeled agent [ 60 ]. The calculated values of ratio of (tumor:blood) (T/B) and ratio of (Tumor: Normal muscle) (T/NM) were; 1.66 and 2.75 at 15 and 30 min p.i, respectively Table 6 .…”

Section: Resultsmentioning

confidence: 99%

Discovery of New Coumarin-Based Lead with Potential Anticancer, CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR, Molecular Dynamics, In Vitro Cytotoxicity, Radioiodination, and Biodistribution Studies

et al. 2021

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Novel 6-bromo-coumarin-ethylidene-hydrazonyl-thiazolyl and 6-bromo-coumarin-thiazolyl-based derivatives were synthesized. A quantitative structure activity relationship (QSAR) model with high predictive power r2 = 0.92, and RMSE = 0.44 predicted five compounds; 2b, 3b, 5a, 9a and 9i to have potential anticancer activities. Compound 2b achieved the best ΔG of –15.34 kcal/mol with an affinity of 40.05 pki. In a molecular dynamic study 2b showed an equilibrium at 0.8 Å after 3.5 ns, while flavopiridol did so at 0.5 Å after the same time (3.5 ns). 2b showed an IC50 of 0.0136 µM, 0.015 µM, and 0.054 µM against MCF-7, A-549, and CHO-K1 cell lines, respectively. The CDK4 enzyme assay revealed the significant CDK4 inhibitory activity of compound 2b with IC50 of 0.036 µM. The selectivity of the newly discovered lead compound 2b toward localization in tumor cells was confirmed by a radioiodination biological assay that was done via electrophilic substitution reaction utilizing the oxidative effect of chloramine-t. 131I-2b showed good in vitro stability up to 4 h. In solid tumor bearing mice, the values of tumor uptake reached a height of 5.97 ± 0.82%ID/g at 60 min p.i. 131I-2b can be considered as a selective radiotheranostic agent for solid tumors with promising anticancer activity.

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“…This leads to the DPP-4 suppression effect, blocking the inactivation of the incretin hormones with the consequent stimulation of insulin secretion and inhibition of glucagon secretion, leading to the control of the glucose level in the body. [75][76][77][78][79][80][81][82][83] In addition, it was clear that the excretion pathway of the 131 I-SQ compound is through the renal route. Moreover, it did not show any high accumulation in other body organs.…”

Section: In Vivo Pharmacokinetic Distribution Of the 131 I-sq Compoundmentioning

confidence: 99%

New quinoxaline compounds as DPP-4 inhibitors and hypoglycemics: design, synthesis, computational and bio-distribution studies

et al. 2021

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Radioiodinated doxorubicin as a new tumor imaging model: preparation, biological evaluation, docking and molecular dynamics

Cited by 20 publications

References 57 publications

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator

Discovery of New Coumarin-Based Lead with Potential Anticancer, CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR, Molecular Dynamics, In Vitro Cytotoxicity, Radioiodination, and Biodistribution Studies

New quinoxaline compounds as DPP-4 inhibitors and hypoglycemics: design, synthesis, computational and bio-distribution studies

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