Preparation of radioiodinated ritodrine as a potential agent for lung imaging

Rashed, Hassan M.; Ibrahim, I. T.; Motaleb, M. A.; El-Bary, A. Abd

doi:10.1007/s10967-014-3077-2

Cited by 35 publications

(7 citation statements)

References 22 publications

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“…All mice organs/tissues were dissected, washed with normal saline, made free from adhering tissue/fluid, and weighed. A sample of mice blood was separated, weighed, and counted for its radioactivity uptake and the total blood radioactivity level was calculated considering blood to constitute 7% of total mice weight (Ding et al, 2012 ; Motaleb et al, 2012 ; Rashed et al, 2014 ). The radioactivity of each organ/tissue as well as the background was counted in a well-type NaI (Tl) crystal coupled to SR-7 scaler ratemeter (Motaleb et al, 2012 ; Rashed et al, 2014 ).…”

Section: Methodsmentioning

confidence: 99%

“…A sample of mice blood was separated, weighed, and counted for its radioactivity uptake and the total blood radioactivity level was calculated considering blood to constitute 7% of total mice weight (Ding et al, 2012 ; Motaleb et al, 2012 ; Rashed et al, 2014 ). The radioactivity of each organ/tissue as well as the background was counted in a well-type NaI (Tl) crystal coupled to SR-7 scaler ratemeter (Motaleb et al, 2012 ; Rashed et al, 2014 ). Percent injected dose per gram (%ID/g ± SD) in a population of three mice for each time point are reported.…”

Section: Methodsmentioning

confidence: 99%

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Contribution of both olfactory and systemic pathways for brain targeting of nimodipine-loaded lipo-pluronics micelles: in vitro characterization and in vivo biodistribution study after intranasal and intravenous delivery

2017

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Nimodipine (NM) is the only FDA-approved drug for treating subarachnoid hemorrhage induced vasospasm. NM has poor oral bioavailability (5-13%) due to its low aqueous solubility, and extensive first pass metabolism. The objective of this study is to develop radiolabeled NMloaded LPM and to test its ability prolong its circulation time, reduce its frequency of administration and eventually target it to the brain tissue. NM was radiolabeled with 99m Tc by direct labeling method using sodium dithionite. Different reaction conditions that affect the radiolabeling yield were studied. The in vivo pharmacokinetic behavior of the optimum NMloaded LPM formulation in blood, heart, and brain tissue was compared with NM solution, after intravenous and intranasal administration. Results show that the radioactivity percentage (%ID/ g) in the heart of mice following administration of 99m Tc-NM loaded LPM were lower compared with that following administration of 99m Tc-NM solution, which is greatly beneficial to minimize the cardiovascular side effects. Results also show that the %ID/g in the blood, and brain following intravenous administration of 99m Tc-NM-loaded LPM were higher at all sampling intervals compared with that following intravenous administration of 99m Tc-NM solution. This would be greatly beneficial for the treatment of neurovascular diseases. The drug-targeting efficiency of NM to the brain after intranasal administration was calculated to be 1872.82%. The significant increase in drug solubility, enhanced drug absorption and the long circulation time of the NM-loaded LPM could be promising to improve nasal and parenteral delivery of NM.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Contribution of both olfactory and systemic pathways for brain targeting of nimodipine-loaded lipo-pluronics micelles: in vitro characterization and in vivo biodistribution study after intranasal and intravenous delivery

2017

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“…The weight of the individual tissue/organ was determined. The radioactivity of each sample as well as the background was counted in a well-type NaI (Tl) crystal coupled to SR-7 scaler ratemeter (Motaleb et al, 2011(Motaleb et al, , 2012Rashed et al, 2014). Percent injected dose per gram (%ID/ g ± S.D.)…”

Section: Bio-distribution Studiesmentioning

confidence: 99%

Trans-nasal zolmitriptan novasomes: in-vitro preparation, optimization and in-vivo evaluation of brain targeting efficiency

et al. 2016

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Migraine attack is a troublesome physiological condition associated with throbbing, intense headache, in one half of the head. Zolmitriptan is a potent second-generation triptan, prescribed for patients with migraine attacks, with or without an aura, and cluster headaches. The absolute bioavailability of zolmitriptan is about 40% for oral administration; due to hepatic first metabolism. Nasal administration would circumvent the pre-systemic metabolism thus increasing the bioavailability of zolmitriptan. In addition, due to the presence of microvilli and high vasculature, the absorption is expected to be faster compared to oral route. However, the bioavailability of nasal administered drugs is particularly restricted by poor membrane penetration. Thus, the aim of this work is to explore the potential of novel nanovesicular fatty acid enriched structures (novasomes) for effective and enhanced nasal delivery of zolmitriptan and investigate their nose to brain targeting potential. Novasomes were prepared using nonionic surfactant, cholesterol in addition to a free fatty acid. A 2 3 full factorial design was adopted to study the influence of the type of surfactant, type of free fatty acid and ratio between the free fatty acid and the surfactant on novasomes properties. The particle size, entrapment efficiency, polydispersity index, zeta potential and % zolmitriptan released after 2 h were selected as dependent variables. Novasomes were further optimized using Design Expert Õ software (version 7; Stat-Ease Inc., Minneapolis, MN), and an optimized formulation composed of Span Õ 80:Cholesterol:stearic acid (in the ratio 1:1:1) was selected. This formulation showed zolmitriptan entrapment of 92.94%, particle size of 149.9 nm, zeta potential of À55.57 mV, and released 48.43% zolmitriptan after 2 h. The optimized formulation was further examined using transmission electron microscope, which revealed non-aggregating multi-lamellar nanovesicles with narrow size distribution. DSC, XRD examination of the optimized formulation confirmed that the drug have been homogeneously dispersed throughout the novasomes in an amorphous state. In-vivo bio-distribution studies of 99m Tc radio-labeled intranasal zolmitriptan loaded novasomes were done on mice, the pharmacokinetic parameters were compared with those following administration of intravenous 99m Tc-zolmitriptan solution. Results revealed the great enhancement in zolmitriptan targeting to the brain, with drug targeting potential of about 99% following intranasal administration of novasomes compared with the intravenous drug solution. Zolmitriptan loaded novasomes administered via the nasal route may therefore constitute an advance in the management of acute migraine attacks.

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“…To quench the reaction, a drop of sodium thiosulfate solution (30 mg/mL H 2 O) was added to convert excess iodine (I 2 ) to iodide (I -) as it is oxidized to tetrathionate (S 4 O 6 ) 2before calculating the radiochemical yield. [47] Different amount of CAT (50, 70, 100, 150, and 200 µg) and drug amounts (50, 100, 150, 200 and 300 µg) are studied while studying the various reaction conditions over the different wide pH range…”

Section: Radioiodination Of Dvsmentioning

confidence: 99%

Novel radioiodinated desvenlafaxine‐loaded lipid nanocapsule for brain delivery

Ayoub,

Abdel‐Mottaleb,

Ibrahem

et al. 2023

Archiv der Pharmazie

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Lipid nanocapsules (LNCs) are lipid nanocarriers developed for drug delivery enhancement. The antidepressant drug desvenlafaxine (DSV) was entrapped in LNC to improve its brain delivery. Different DSV‐loaded LNCs formulae using different oils and surfactants were studied to obtain the optimum formula for further studies. In vivo biodistribution studies were done using Swiss albino mice by intravenous injection of DSV‐loaded LNCs by radioiodination technique. The optimum DSV‐loaded LNC formula was obtained by using Labrafil® M1944CS as the oil and Solutol® HS15 as the surfactant in the ratio of 1:1, with a particle size of 34.28 ± 0.41 nm, a polydispersity index of 0.032 ± 0.05, a zeta potential of −25.77 ± 1.41, and good stability for up to 6 months. The in vivo biodistribution and pharmacokinetics data ensure the bioavailability improvement for DSV brain delivery as Cmax and AUC(1–t) increased more than double for intravenously DSV‐loaded LNCs compared with the DSV solution. In conclusion, the results obtained from this study give an insight into the great potential of using DSV‐loaded LNC for the enhancement of brain delivery.

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Preparation of radioiodinated ritodrine as a potential agent for lung imaging

Cited by 35 publications

References 22 publications

Contribution of both olfactory and systemic pathways for brain targeting of nimodipine-loaded lipo-pluronics micelles: in vitro characterization and in vivo biodistribution study after intranasal and intravenous delivery

Contribution of both olfactory and systemic pathways for brain targeting of nimodipine-loaded lipo-pluronics micelles: in vitro characterization and in vivo biodistribution study after intranasal and intravenous delivery

Trans-nasal zolmitriptan novasomes: in-vitro preparation, optimization and in-vivo evaluation of brain targeting efficiency

Novel radioiodinated desvenlafaxine‐loaded lipid nanocapsule for brain delivery

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