Gold nanoparticles for 99mTc-doxorubicin delivery: formulation, in vitro characterization, comparative studies in vivo stability and biodistribution

El-Safoury, D. M.; Ibrahim, A. B.; El-Setouhy, Doaa Ahmed; Khowessah, Omneya Mohammed; Motaleb, M. A.; Sakr, Tamer M.

doi:10.1007/s10967-021-07633-y

Cited by 9 publications

(3 citation statements)

References 59 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The in-vivo stability of the developed 99m Tc-ZT complex was confirmed by its low stomach uptake after oral administration of 99m Tc-ZT solution and transdermal application of 99m Tc-ZT-T6 gel [ 18 , 47 ]. The 99m Tc-ZT uptakes in brain, blood and liver were estimated, at predesigned time intervals up to 24 h, that were equivalent to the ZT concentrations in organs or fluid.…”

Section: Resultsmentioning

confidence: 99%

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by 99mTc radiolabeling technique

Tawfik,

Eltaweel,

Fatouh

et al. 2023

Drug Deliv. and Transl. Res.

Self Cite

View full text Add to dashboard Cite

Zolmitriptan (ZT) is a potent second generation triptan, commonly administered to alleviate migraine attacks. ZT suffers various limitations; massive hepatic first pass metabolism, P-gp efflux transporters susceptibility, and limited (≈40%) oral bioavailability. Transdermal route of administration could be explored to enhance its bioavailability. A 23.31 full factorial design was constructed to developed twenty-four ZT loaded terpesomes via thin film hydration technique. The influence of drug: phosphatidylcholine ratio, terpene type, terpene concentration and sodium deoxycholate concentration on the characterization of the developed ZT-loaded terpesomes was assessed. Particle size (PS), zeta potential (ZP), ZT entrapment efficiency (EE%), drug loading (DL%) and drug released percentages after 6 h (Q6h) were the selected dependent variables. Further morphological, crystallinity, and in-vivo histopathological studies were conducted for the optimum terpesomes (T6). 99mTc-ZT and 99mTc-ZT-T6 gel were radio-formulated for in-vivo biodistribution studies in mice following transdermal application of 99mTc-ZT-T6 gel, relative to 99mTc-ZT oral solution. T6 terpesomes [comprising ZT and phosphatidylcholine (1:15), cineole (1% w/v) and sodium deoxycholate (0.1% w/v)] were optimum with respect to spherical PS (290.2 nm), ZP (-48.9 mV), EE% (83%), DL% (3.9%) and Q6h (92.2%) with desirability value of 0.85. The safety of the developed T6 terpesomes was verified by the in-vivo histopathological studies. 99mTc-ZT-T6 gel showed maximum brain concentration (5 ± 0.1%ID/ g) with highest brain to blood ratio of 1.92 ± 0.1 at 4 h post transdermal application. Significant improvement of ZT brain relative bioavailability (529%) and high brain targeting efficiency (315%) were revealed with 99mTc-ZT-T6 gel, which confirmed successful ZT delivery to the brain. Terpesomes could be safe, successful systems capable of improving ZT bioavailability with high brain targeting efficiency. Graphical Abstract

show abstract

Section: Resultsmentioning

confidence: 99%

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by 99mTc radiolabeling technique

Tawfik,

Eltaweel,

Fatouh

et al. 2023

Drug Deliv. and Transl. Res.

Self Cite

View full text Add to dashboard Cite

show abstract

“…International Journal of Nanomedicine 2023:18 1582 or therapy) and nanoformulations to formulate nano radiopharmaceutical become an urgent necessity to be used as a theragnostic agent. 42 Preparation of Radioiodinated Clozapine ([ 131 I] Iodo-CLZ) CLZ radioiodination was performed using the oxidizing agent chloramine-T (CAT) 43 with 10 μL of Na 131 I (30 MBq). The parameters with an impact on the radioiodination yield were investigated, such as CLZ concentration (0.2-1.6 mg/mL), CAT concentration (50-250 µg/mL), pH range (3-10) and the reaction duration (5-60 min).…”

Section: Dovepressmentioning

confidence: 99%

Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation

Elsharkawy¹,

Amin²,

Shamsel-Din³

et al. 2023

IJN

Self Cite

View full text Add to dashboard Cite

The research objective is to design intranasal brain targeted CLZ loaded lecithin based polymeric micelles (CLZ-LbPM) aiming to improve central systemic CLZ bioavailability. Methods: In our study, intranasal CLZ loaded lecithin based polymeric micelles (CLZ-LbPM) were formulated using soya phosphatidyl choline (SPC) and sodium deoxycholate (SDC) with different CLZ:SPC:SDC ratios via thin film hydration technique aiming to enhance drug solubility, bioavailability and nose to brain targeting efficiency. Optimization of the prepared CLZ-LbPM using Design-Expert® software was achieved showing that M6 which composed of (CLZ:SPC: SDC) in respective ratios of 1:3:10 was selected as the optimized formula. The optimized formula was subjected to further evaluation tests as, Differential Scanning Calorimetry (DSC), TEM, in vitro release profile, ex vivo intranasal permeation and in vivo biodistribution. Results:The optimized formula with the highest desirability exhibiting (0.845), small particle size (12.23±4.76 nm), Zeta potential of (−38 mV), percent entrapment efficiency of > 90% and percent drug loading of 6.47%. Ex vivo permeation test showed flux value of 27 μg/cm².h and the enhancement ratio was about 3 when compared to the drug suspension, without any histological alteration. The radioiodinated clozapine ([ 131 I] iodo-CLZ) and radioiodinated optimized formula ([ 131 I] iodo-CLZ-LbPM) were formulated in an excellent radioiodination yield more than 95%. In vivo biodistribution studies of [ 131 I] iodo-CLZ-LbPM showed higher brain uptake (7.8%± 0.1%ID/g) for intranasal administration with rapid onset of action (at 0.25 h) than the intravenous formula. Its pharmacokinetic behavior showed relative bioavailability, direct transport percentage from nose to brain and drug targeting efficiency of 170.59%, 83.42% and 117% respectively. Conclusion:The intranasal self-assembling lecithin based mixed polymeric micelles could be an encouraging way for CLZ brain targeting.

show abstract

“…Inorganic NPs can be chemically synthesized using several different techniques such as co-precipitation, hydrothermal, combustion, sol-gel, chemical reduction, chemical vapor and microwave-assisted methods [ 67 , 68 , 69 , 70 , 71 ]. In this review, we present inorganic NPs that are synthesized using reducing and stabilizing agents where the reducing agent is responsible for the reduction of the metal from high oxidation states (+3, +2 or +1) to its metallic form (zero oxidation state), while the stabilizing agent is responsible for surface stabilization of metal nano materials [ 22 , 42 , 44 , 45 , 47 , 49 , 50 , 52 ]. Various NPs including AuNPs, selenium nanoparticles (SeNP), iron nanoparticles (FeNP), copper nanoparticles (CuNP) and silver nanoparticles (AgNP) were evaluated for their effective delivery of different radionuclides such as tecnetium-99m (Tc-99m), iodine-131 (I-131) and gold-198 (Au-198) to tumor sites for tumor theranostics [ 42 , 44 , 45 , 47 , 48 , 49 , 50 , 51 , 52 , 72 ].…”

Section: Design and Development Of Nanoparticlesmentioning

confidence: 99%

IAEA Contribution to Nanosized Targeted Radiopharmaceuticals for Drug Delivery

et al. 2022

Self Cite

View full text Add to dashboard Cite

The rapidly growing interest in the application of nanoscience in the future design of radiopharmaceuticals and the development of nanosized radiopharmaceuticals in the late 2000′s, resulted in the creation of a Coordinated Research Project (CRP) by the International Atomic Energy Agency (IAEA) in 2014. This CRP entitled ‘Nanosized delivery systems for radiopharmaceuticals’ involved a team of expert scientist from various member states. This team of scientists worked on a number of cutting-edge areas of nanoscience with a focus on developing well-defined, highly effective and site-specific delivery systems of radiopharmaceuticals. Specifically, focus areas of various teams of scientists comprised of the development of nanoparticles (NPs) based on metals, polymers, and gels, and their conjugation/encapsulation or decoration with various tumor avid ligands such as peptides, folates, and small molecule phytochemicals. The research and development efforts also comprised of developing optimum radiolabeling methods of various nano vectors using diagnostic and therapeutic radionuclides including Tc-99m, Ga-68, Lu-177 and Au-198. Concerted efforts of teams of scientists within this CRP has resulted in the development of various protocols and guidelines on delivery systems of nanoradiopharmaceuticals, training of numerous graduate students/post-doctoral fellows and publications in peer reviewed journals while establishing numerous productive scientific networks in various participating member states. Some of the innovative nanoconstructs were chosen for further preclinical applications—all aimed at ultimate clinical translation for treating human cancer patients. This review article summarizes outcomes of this major international scientific endeavor.

show abstract

Gold nanoparticles for 99mTc-doxorubicin delivery: formulation, in vitro characterization, comparative studies in vivo stability and biodistribution

Cited by 9 publications

References 59 publications

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by 99mTc radiolabeling technique

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by 99mTc radiolabeling technique

Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation

IAEA Contribution to Nanosized Targeted Radiopharmaceuticals for Drug Delivery

Contact Info

Product

Resources

About