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This study aimed to synthesize a new pyrimidine derivative with a good synthesis yield of 87% to act as a new cancer marker after radiolabeling with Tc-99m in a high radiochemical yield of 92.3%. In-vivo study in tumor-bearing Swiss albino mice model revealed promising data with high uptake in cancer. Docking study showed good binding interactions of the radiosynthesized complex at the binding site. In conclusion, this novel complex could be a potential probe for cancer targeting.

As the 'Resveratrol was radiolabeled with radioactive iodine where the radioiodination efficiency was enlightened and the computational approaches were employed to investigate the affinity and specificity with tubulins. Furthermore, the in-vivo distribution and pharmacokinetic studies in normal and tumor induced mice were investigated.The maximum radioiodination yield (94.6 ± 1.66) was achieved at optimum preparation parameters stated as 100 μg/mL of oxidizing agent, 100 μg/ml of resveratrol, reaction time of 30 min and reaction pH 5. The in silico studies showed that di-iodinated resveratrol (compound 6) exhibited the best binding score (-34.46) and interaction with the β-tubulin binding site. The in vivo distribution in tumor models revealed a significant accumulation (4.02% ID/g) in tumor lesion at 60 min p.i. The rate of drug elimination demonstrated a mono-exponential decline of radioactivity versus time in the blood.Radioiodinated resveratrol revealed good microtubules targeting which render it as a novel theranostic probe for cancer management.

Nanoparticles are frequently used as targeting delivery systems for therapeutic and diagnostic radiopharmaceuticals. Polyethylene oxide-polyacrylic acid (PEO-PAAc) nanogel was prepared via γ-radiation-induced polymerization. Variable factors affecting nanoparticles size were investigated. The nanogel was radiolabeled with the imaging radioisotope 99m Tc and finally conjugated with folic acid to target folate receptor actively. PEO-PAAc-folic acid gel was characterized by dynamic light scattering (DLS) and atomic force microscopy (AFM). Biodistribution was studied in normal mice and solid tumor-bearing mice via intravenous and intratumor injections of the radiolabeled PEO-PAAc-folic acid nanogel. Results of biodistribution showed high selective uptake of the prepared complex in tumor muscle compared with normal muscle for both intravenous and intratumor injections. The T/NT ratio was found to be 6.186 and 294.5 for intravenous and intratumor injections, respectively. Consequently, 99m Tc-PEO-PAAc-folic acid complex could be a promising agent for cancer diagnostic imaging.

Gold nanoparticles (AuNPs) represent very attractive and promising drug delivery carriers due to their unique dimensions, adjustable surface functions, and controllable drug release. Therefore, AuNPs are used to overcome the limitations of conventional chemotherapy, for example methotrexate (Mex), one of the first-generation chemotherapy drugs for cancer treatment, whose usefulness has been restricted due to drug resistance and dose-dependent side effects. In the present study, the AuNPs drug delivery system was synthesized and loaded with technetium-99 m radiolabeled Methotrexate (99mTc-Mex) to produce new potential nanoradiopharmaceutical for tumor targeting and further imaging. The Methotrexate loaded gold nanoparticles (Mex-AuNPs) successfully prepared in small spherical particle size (20.3 nm), polydispersity index PDI ( 90 %. The preclinical biodistribution studies of 99mTc-Mex-AuNPs were performed in 3 experimental groups A (intravenous (I.V.) injected normal mice), B and C (I.V. and intratumor (I.T.) injected tumor bearing mice, respectively). The 99mTc-Mex-AuNPs achieved highest tumor uptake (93 ± 0.39 %ID/g) and highest Target/NonTarget (T/NT) ratio (58.1 ± 0.91) with high Tumor/Blood (T/B) ratio (25.8 ± 0.11) at 10 min post I.T. injection and retained high tumor uptake (79 ± 0.65 %ID/g) up to 60 min post I.T. injection before escaping into blood stream. Consequently, 99mTc-Mex-AuNPs can be considered as new potential nanoradiopharmaceutical in tumor diagnosis.

This study was designed to biosynthesize Aspergillus flavus copper oxide NPs (AFCuONPs) using extracellular fungous filtrate technique and evaluating its medical importance. AFCuONPs were successfully biosynthesized with average size of 32.4 nm and zeta potential of – 36 mV. They were fully characterized using FT-IR, UV–Vis spectrophotometry, and TEM. AFCuONPs cytotoxicity and bactericidal activity were evaluated against different cell lines and pathogenic bacteria, respectively. [99mTc]Tc-AFCuONPs were radiosynthesized with high radiolabeling yield (93 ± 0.85%). In vivo biodistribution of [99mTc]Tc-AFCuONPs in tumor-bearing mice model showed high tumor uptake. These results introduce AFCuONPs as a promising medical agent.

The [99mTc]Tc-Doxorubicin–Gold Nanoparticles (99mTc-Dox-AuNPs) was formulated as a nanoradiopharmaceutical by different loading procedures to enhance tumor targeting. The formula F1 that was prepared by direct loading of pre-prepared [99mTc]Tc-Doxorubicin showed a reasonable in-vitro characterization values, high entrapment efficiency (92 ± 0.72%), acceptable in vitro release data and convenient in-vitro serum stability up to 24 h. F1 presented high tumor uptake (54%ID/g) with high Target/ Non Target (T/NT) ( ≈ 77) and Drug Target Efficiency percent (%DTE) above 100% at 0.5 h via intra-tumoral injection that prove the increasing of tumor targeting and in-vivo stability by direct loading for pre-prepared [99mTc]Tc-Doxorubicin.

The current work represents the design and synthetic approaches of a new set of compounds 6–10 bearing the 1,4-dimethyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide scaffold. The biological evaluation revealed that most of the new compounds were promising selective dipeptidyl peptidase-IV (DPP-4) inhibitors and in vivo hypoglycemic agents utilizing linagliptin as a standard drug. The acute toxicity examination confirmed the safety profile of all compounds. Molecular docking studies related the significant DPP-4 suppression activity of compounds 9a, 10a, 10f, 10g to their nice fitting in the active pocket of DPP-4. In addition, the molecular dynamic study exhibited the stability of both 10a and 10g within the active site of DPP-4. The QSAR study showed that the difference between the predicted activities is very close to the experimental suppression effect. Moreover, both compounds 10a and 10g obeyed Lipinski's rule, indicating their efficient oral bioavailability. Compound 10a was radiolabeled, forming the 131I-SQ compound 10a to study the pharmacokinetic profile of this set of compounds. The biodistribution pattern hit the target protein since the tracer accumulated mainly in the visceral organs where DPP-4 is secreted in a high-level, thus with consequent stimulation of insulin secretion, leading to the target hypoglycemic effect.

Targeted drug delivery system can reduce the side effects of high drug concentration by improving drug pharmacokinetics at lower doses. Citrate-gold nanoparticles (AuNPs) as a drug delivery system were synthesized via green nanotechnology technique to be used as a new imaging platform for tumor targeting. Citrate-AuNPs were synthesized with core size of 10 nm. Citrate-AuNPs were labeled with technetium-99m (99mTc) with radiochemical yield of 95.20 ± 2.70% with good in-vitro stability in both saline and human serum and well in-vivo studied in both normal and solid tumor bearing mice. The in-vivo biodistribution study of [99mTc]Tc-citrate-AuNPs in solid tumor bearing mice (as preliminary study) showed a high accumulation in tumor site with tumor/muscle of 4.35 ± 0.22 after 30 min post injection. The direct intratumoral (I.T) injection of [99mTc]Tc-citrate-AuNPs showed that this complex was retained in the tumor up to 77.86 ± 1.90 % at 5 min and still around 50.00 ± 1.42 % after 30 min post injection (p.i.). The newly presented nano-platform could be presented as a new potential radiopharmaceutical tumor imaging probe.

This study aimed to develop a simple method for synthesis of vitamin c-coated selenium nanoparticles which were then labeled with technetium-99m for further in vivo studies on normal and solid tumor induced mice. Results showed the formation of amorphous SeNPs with a mean size of (23 ± 5 nm). The radiolabelling yield of [99mTc-Vit_C (SeNPs)] was (96 ± 2%) with stability up to 6 h. Effective target non-target ratios were obtained in solid tumor-induced mice throughout the experimental time points. [99mTc-Vit_C (SeNPs)] complex showed promising features which make it a potential radiopharmaceutical for imaging of solid tumors.

The present work describes a quinazolinone-based lead optimization for the development of novel purine nucleoside phosphorylase (PNP) inhibitors with quinazolinone scaffold. Nineteen compounds were proposed and docked against PNP, the best 14 compounds with highest docking and affinity scores and low RMSD values were synthesized. Synthesis of new quinazolinone derivatives with variable acetamide substituents on two positions on quinazoline ring was performed. The structures assigned to the products were concordant with the microanalytical and spectral data. In vitro cytotoxicity on human breast cancer cell line (MCF7) was performed and identified compound 6g as the most potent with IC

Background: 5-azacitidine is a very potent chemotherapeutic agent that suffers from certain limitation. Objective: This study aims to prepare gold nanoparticles as a new nano-formula of 5-azacitidine that can improve its bioavailability and decrease its side effects. Methods: 5-azacytidine loaded GA-AuNPs were prepared and characterized by UV-Vis spectroscopy, infrared (IR) and transmission electronic microscope (TEM). This new platform was characterized in vitro by measuring its zeta potential, particle size, drug loading efficacy and its anti-proliferative effect on MCF-7 cell line was evaluated. In vivo biodistribution studies of 99mTc-5-aza solution and 99mTc-5-aza-gold nano formula were conducted in tumor bearing mice by different routes of administration (Intravenous and Intra-tumor). Results: 5-Aza-GA-AuNPs formula was successfully prepared with optimum particle size of ≈34.66 nm, zeta potential of -14.4 mV and high entrapment efficiency. 99mTc-5-Aza-GA-AuNPs was efficient radiosynthesized (95.4%). Biodistribution studies showed high selective accumulation in tumor and low uptake in non-target organs in case of 5-Aza-GA-AuNPs formula than 99mTc-5-azacitidine solution. Conclusion: 99mTc-5-Aza-GA-AuNPs had succeeded to improve the selectivity and uptake of 5-azacitidine in cancer. Moreover, 99mTc-5-Aza-GA-AuNPs could be used as a hopeful theranostic radiopharmaceutical preparation for cancer.

This study aimed to synthesize a nano-structure between selenium, Vit. C, and Vit. E (Vit-E/C@SeNPs) as a promising protective and therapeutic agent for hepatocellular carcinoma. Vit-E/C@SeNPs were characterized using TEM and DLS and its zetapotential was measured to evaluate its stability. DPPH assay and SRB test were performed to estimate its antioxidant capacity and cytotoxicity, respectively. A radiosynthesis of 99mTc-Vit-E/C@SeNPs was done for further in-vivo pharmacokinetic studies on normal and solid tumor induced mice. Further, in-vivo studies were conducted to investigate Vit-E/C@SeNPs efficacy against hepatocellular damage in Wistar albino rats induced by diethylnitrosamine (DEN) / Carbon Tetra chloride (CCl4). The synthesis results showed spherical Vit-E/C@SeNPs with core size of 50 nm, radical scavenging activity (%RSC) of 75.9%, and IC50 of 27.9 µg/ml. The biochemical analysis results showed that the lower liver function biomarker values (ALT, AST, ALP, total bilirubin and GGT) has gone for the Vit-E/C@SeNPs prevention and treated group, which also showed significant depletion of liver tissue l -MDA, and obvious increase in GSH concentration and CAT activity and marked improvement in the histological feature of liver tissue. Additionally, a significant up-regulation of mRNA gene expression levels of inflammatory gene (TGFβ1, NFκB, iNOS, PPAR-γ and TNFα) and Apoptotic gene (P53) were determined by using Quantitative real-time PCR (qPCR). The values down regulate and tend to normal in prevention and control group. All of these introduce Vit-E/C@SeNPs as a promising agent as protective and therapeutic agent against DEN/ CCl4-induced hepatocellular damage (Hepatocellular carcinoma).

Nanoparticles are frequently used as targeting delivery systems for therapeutic and diagnostic radiopharmaceuticals. Polyethylene oxide-polyacrylic acid (PEO-PAAc) nanogel was prepared via γ-radiation-induced polymerization. Variable factors affecting nanoparticles size were investigated. The nanogel was radiolabeled with the imaging radioisotope

Graphene is a crystalline form of carbon that is regarded as a novel and innovative product. carboxylated nanographene oxide sheets (NGO-COOH) was synthesized using a modified Hummer's method and assess their medical significance. NGO-COOH were successfully synthesized with an average size of 40 nm. FT-IR, UV–Vis, XPS spectrophotometry, and TEM were used to thoroughly describe them. The cytotoxicity function of NGO-COOH nanosheets were tested against cell line. The radiosynthesized [99mTc]Tc-NGO-COOH had a high radiolabeling yield (97.3±0.45 %). The tumor uptake of [99mTc]Tc-NGO-COOH nanosheets in an in vivo biodistribution model in tumor-bearing mice was high. NGO-COOH nanosheets may be a promising imaging agent, based on these findings.

PURPOSE: Oral administration of Iodine(−131) (I(−131)) solutions causes high risk of contamination for patients and dispensers. The objective of the study was to adapt hard gelatin capsules (HGCs) for filling with radiopharmaceutical solutions without deformation. METHODS: Polystyrene (PS) internally lining films with different thicknesses were used to protect HGCs. The insulated HGCs were evaluated for their physicochemical characteristics and rupturing time in different dissolution media. HGCs internally lined with PS were examined for withstand loading with different volumes and radioactivities of I(−131) solutions. Radioactivity release was studied in deionized water and acidic media. Quality control of released I(−131) was inspected for radiochemical purities. RESULTS: There was a directly proportion between PS lining thickness and stability of HGCs after filling with 500 μl aqueous methylene blue solution. HGCs internally lined with PS 100 μm thickness withstand deformation for ˃ two months; however showed fast in-vitro rupturing time in different dissolution media. Internally lined HGCs loaded with different volumes and radioactivities of I(−131) solutions resisted for one week without radioactive leakage. Yet, revealed complete release of I(−131) after 20 min in dissolution media with great radiochemical purity. CONCLUSION: The study promises safely I(−131) aqueous solution delivery via adapted HGCs. [Figure: see text]

Curcumin is a polyphenol extracted from Curcuma longa, used as a spice, in food coloring, and as a traditional herbal medicine. It has wide therapeutic platform as anti-oxidant, anticancer, anti-inflammatory and anti-infection properties. This review discusses the analytical methods used in determination of curcumin in various matrices with degradation profile, expected degradation products and stability tests.

Urease enzyme is a virulence factor that helps in colonization and maintenance of highly pathogenic bacteria in human. Hence, the inhibition of urease enzymes is well-established to be a promising approach for preventing deleterious effects of ureolytic bacterial infections. In this work, novel thiobarbiturate derivatives were synthesized and evaluated for their urease inhibitory activity. All tested compounds effectively inhibited the activity of urease enzyme. Compounds 1, 2a, 2b, 4 and 9 displayed remarkable anti-urease activity (IC50 = 8.21–16.95 μM) superior to that of thiourea reference standard (IC50 = 20.04 μM). Moreover, compounds 3a, 3g, 5 and 8 were equipotent to thiourea. Among the tested compounds, morpholine derivative 4 (IC50 = 8.21 µM) was the most potent one, showing 2.5 folds the activity of thiourea. In addition, the antibacterial activity of the synthesized compounds was estimated against both standard strains and clinical isolates of urease producing bacteria. Compound 4 explored the highest potency exceeding that of cephalexin reference drug. Moreover, biodistribution study using radiolabeling approach revealed a remarked uptake of 99mTc-compound 4 into infection induced in mice. Furthermore, a molecular docking analysis revealed proper orientation of title compounds into the urease active site rationalizing their potent anti-urease activity.

Selenium nanoparticles (SeNPs) have become one of the most prospective and promising tools in the course of cancer diagnosis and therapy. Here we describe the synthesis of a novel radioactive platform for tumor imaging using selenium nanoparticles. SeNPs were synthetized using dithionite and glutathione as reducing and capping agent respectively with 5 mmol/L sodium selenite as a precursor and then SeNPs radiolabeled with technetium-99 m, the most common and famous radioactive isotope used for imaging purposes. A characteristic profile for the synthesized SeNPs was performed including size analysis, zeta potential, antioxidant activity, radiochemical yield and in-vivo biodistribution in normal and solid tumor bearing mice. Size analysis showed amorphous SeNP cores of a mean diameter of 21 ± 5 nm with a hydrodynamic size of 43 ± 8 nm and −28 mV zeta potential. The particles also showed a superior antioxidant activity of radical scavenging activity 55.6% according to DPPH assay, in addition, satisfying radiochemical yield up to 97 ± 1.5 was achieved. In vivo studies were applied on male Swiss albino mice that demonstrated a good biodistribution pattern in normal mice with a moderate accumulation in liver at 30 min post injection. Excellent T/NT ratios were obtained in solid tumor bearing mice throughout the experimental time points. The as-synthetized selenium nanoparticles demonstrated surprising and satisfying features which make them promising enough for tumor theranosis.

We report herein an innovative approach to prostate tumor therapy using tumor specific radioactive gold nanoparticles (198Au) functionalized with Mangiferin (MGF). Production and full characterization of MGF-198AuNPs are described. In vivo therapeutic efficacy of MGF-198AuNPs, through intratumoral delivery, in SCID mice bearing prostate tumor xenografts are described. Singular doses of the nano-radiopharmaceutical (MGF-198AuNPs) resulted in over 85% reduction of tumor volume as compared to untreated control groups. The excellent anti-tumor efficacy of MGF-198AuNPs are attributed to the retention of over 90% of the injected dose within tumors for long periods of time. The retention of MGF-198AuNPs is also rationalized in terms of the higher tumor metabolism of glucose which is present in the xanthanoid functionality of MGF. Limited/no lymphatic drainage of MGF-198AuNPs to various non-target organs is an attractive feature presenting realistic scope for the clinical translation of MGF-198AuNPs in for treating prostate cancers in human patients. The comparative analysis of MGF-198AuNPs with other radioactive gold nanoparticles, functionalized either with epigallocatechin gallate or the Gum Arabic, has revealed significantly superior tumoricidal characteristics of MGF-198AuNPs, thus corroborating the importance of the tumor-avid glucose motif of MGF. Oncological implications of MGF-198AuNPs as a new therapeutic agent for treating prostate and various solid tumors are presented.

Purpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a pot...

Nanotechnology may be applied in medicine where the utilization of nanoparticles (≤100 nm) for the delivery and targeting of theranostic agents is at the forefront of projects in cancer nano-science. This study points a novel one step synthesis approach to build up polyethylene glycol capped silver nanoparticles doped with I-131 radionuclide (131I-doped Ag-PEG NPs). The formula was prepared with average hydrodynamic size 21 nm, zeta potential - 25 mV, radiolabeling yield 98 ± 0.76%, and showed good in-vitro stability in saline and mice serum. The in-vitro cytotoxicity study of cold Ag-PEG NPs formula as a drug carrier vehicle showed no cytotoxic effect on normal cells (WI-38 cells) at a concentration below 3 μL/104 cells. The in-vivo biodistribution pattern of 131I-doped Ag-PEG NPs in solid tumor bearing mice showed high radioactivity accumulation in tumor tissues with maximum uptake of 35.43 ± 1.12 and 63.8 ± 1.3% ID/g at 60 and 15 min post intravenous (I.V.) and intratumoral injection (I.T.), respectively. Great potential of T/NT ratios were obtained throughout the experimental time points with maximum ratios 45.23 ± 0.65 and 92.46 ± 1.02 at 60 and 15 min post I.V. and I.T. injection, respectively. Thus, 131I-doped Ag-PEG NPs formulation could be displayed as a great potential tumor nano-sized theranostic probe.

Selenium is one of the most important dietary supplements in the human diet. It is incorporated into the synthesis of many antioxidant proteins, which serve as scavengers of reactive oxygen species such as glutathione peroxidase. Therefore, selenium has become antagonistic and resistant to many diseases resulting from oxidative stress such as arthritis, tumors, and heart and brain diseases. Selenium nanoparticles (SeNPs) have the potential to serve as new nutritional supplements with higher degradability, lower toxicity and ability to be cleared gradually from the body. Selenium nanoparticles have emerged as unusual selenium species with amazing prophylactic and therapeutic properties with dual synergistic effects of providing therapeutic cargo and improved anticancer activity. Recent investigations have also explored new applications of nano-scaled forms of selenium for a wide range of biological activities such as antibacterial and antifungal agents. Herein, we provide a focused account on the recent advances on various biomedical applications of selenium nanoparticles with a particular emphasis on their chemistry, nanotechnology and various applications in life sciences.

Non-invasive molecular imaging techniques are accruing more interest in the last decades. Several radiolabelling elements have been FDA-approved and are currently used to characterize tumors. In this study, the DNA intercalating agent doxorubicin was radiolabelled with 125I. Several parameters for the radiolabelling reaction were investigated and optimized. A maximum yield of 94 ± 0.3% was reached after reacting 20 μg of doxorubicin with 200 μg Chloramine-T at pH 5 for 30 min. The in vivo stability of 125I-doxorubicin is validated by the low propensity for thyroid uptake in mice. The preclinical T/NT ratio was approximately 6.4 at 30 min. Docking and molecular dynamics confirmed that the radiolabelling of doxorubicin did not affect (or slightly improved its binding to DNA). Overall, 125I-doxorubicin was demonstrated to be a promising non-invasive probe for solid tumor imaging.

Virus infections are an increasing and probably lasting global risk. Nucleoside and nucleotide analogs represent the largest class of antiviral drugs. Early success in the treatment of human immunodeficiency virus infection and the recent approval of sofosbuvir as phosphoramidate nucleoside prodrug for chronic hepatitis C have provided proof of concept for important this class of compounds as an antiviral agent. This review summarizes the antiviral activity of nucleoside and nucleotide analogs and their recent application.

The aim of the presented study is to investigate a new promising radiopharmaceutical tracer able to visualize and differentiate inflammation versus infection in early stages. Radioiodinated tenoxicam ( 125 I-tenoxicam) was prepared and its radiochemical yield and in vitro stability were assayed. The biodistribution studies were conducted on two different mice models: sterile inflammation and bacterial infection mice models. 125I-tenoxicam showed high T/NT accumulation in the inflammatory tissues revealing high selectivity to the inflammatory tissues in contrast to infection bearing mice. The docking study using CDOCKER protocol for tenoxicam and radioiodinated tenoxicam with COX enzymes was performed to confirm that radioiodinated tenoxicam still retaining COX enzymes selectivity.

The purpose of our investigation was to promote the bioavailability and the brain delivery of rivastigmine tartarate (RV) through optimization of mucoadhesive thermosensitive in situ gel via intranasal (IN) route. The mucoadhesive in situ gels were developed using pluronic F127 (PF127) as thermogelling agent and different mucoadhesive polymers. A full factorial design was implemented to study the influence of three factors; pluronic type at two levels (PF127, PF127/PF68), mucoadhesive polymer type at four levels (HPMC, Chitosan, Carbopol 934 and NaCMC) and mucoadhesive polymer concentration at two levels (0.5 and 1%w/v). The studied responses were sol-gel temperature, consistency, gel strength, adhesion work and T50% of drug release. In vivo pharmacokinetic and biodistribution studies of the selected formula were investigated using radiolabeling approach using normal albino mice. The optimal RV in situ gel (PF127 and 1% Carbopol 934) showed significant transnasal permeation (84%) which was reflected in better distribution to the brain (0.54 %ID/g), when compared to RV IN solution (0.16 %ID/g) and RV IV intravenous solution (0.15 %ID/g). In conclusion, the investigated results showed the potential use of mucoadhesive in situ gel as a promising system for brain targeting of RV via the transnasal delivery system.

Objective: Directly incorporating aqueous solutions into hard gelatin capsules (HGCs) without dispersing them in an oily medium is considered a challenge for most researchers and manufacturers. The aim of the study is to evaluate the effect of gamma radiation (ɣ-radiation) on the adaptation of HGCs for aqueous solution delivery. Methods: Empty HGC shells were exposed to four of ɣ-radiation doses (1, 3, 5, 10 kGy). Then, the physicochemical properties of irradiated capsules were evaluation and compared with those of non-irradiated capsules. Fourier-transform infrared spectroscopy (FT-IR), capsule hardness, and water incorporation tests were performed. In-vitro disintegration/dissolution behavior determined as (rupture time) in different dissolution media was evaluated.Results: The results showed direct proportionality between the ɣ-radiation dose and HGC crosslinking degree up to 3 kGy, while at doses >3 kGy, degradation rather than crosslinking occurred. The results were clearly demonstrated by FTIR as peptide linkages between gelatin molecules.All the ɣ-irradiated HGCs submitted to hardness test were completely deformed without rupture with increasing capsule deformation work (J) for γ-radiation doses up to 3 kGy; the deformation work declined at doses >3 kGy. The water incorporation study revealed that capsules exposed to 3 kGy could hold up to 100 ml of methylene blue solution without deformation or leakage for 45 minutes compared with non-irradiated HGCs, which showed a significantly lower tolerance of only 2 minutes (p

Stem cells are undifferentiated cells with a potential to be developed into different types of body cells. Stem cells are used in regenerative medicine as a repair system that is working to restore the structures and functions of damaged tissues and organs aiming to find a way to cure untreatable injuries and diseases. Stem cell-nanotechnology hybrid is the application of nanotechnology in stem cells research. One of the most interesting applications is the biocompatible magnetically-responsive nanoparticles (NP) that are being utilized for the targeted delivery of stem cells; in order to enhance their retention in the desired treatment site. This review provides an overview of stem cells therapy based on nanotechnology for the treatment of different diseases, such as: peripheral artery disease (PAD), myocardial infarction (MI), atherosclerosis, Huntington's disease, spinal cord injury (SCI), Alzheimer disease (AD), diabetes mellitus (DM), multiple sclerosis (MS), erectile dysfunction (ED), and cancer diseases.

Nanostructured materials attracted considerable attention because of its high surface area to volume ratio resulting from their nano-scale dimensions. This class of sorbents is expected to have a potential impact on enhancement the efficacy of radioisotope generators for diagnostic and therapeutic applications in nuclear medicine. This review provides a summary on the importance of nanostructured materials as effective sorbents for the development of clinical-scale radioisotope generators and outlining the assessment of recent developments, key challenges and promising access to the near future.

The current study is aimed to prepare 99mTc-lidocaine as a new myocardial perfusion-imaging agent. The used 99mTc was obtained from Al–99Mo-molybdate(VI) gel matrix. 99mTc-lidocaine showed higher (15.4 ± 0.11% ID/g) and faster (15 min post injection) cardiac uptake than the recently studied 99mTc-valsartan and 99mTc-procainamide. Consequently, 99mTc-lidocaine will be a valuable myocardial SPECT agent for diagnosis of emergency patients. Besides, the receptor affinity study confirmed the selectivity of 99mTc-lidocaine for sodium channels in the heart.

The presented work describes the efficient use of nano-crystalline titania (TiO2) to remove trace levels of cesium radio-contaminants (134Cs and 137Cs) in iodine-125 (125I) solution produced via neutron activation of natural 124Xe target. The adsorption parameters of TiO2 were investigated to attain the optimum purification and concentration conditions of 125I solution. The maximum sorption capacity of Cs and 125I were approximately 56 and 67 mg/g TiO2, respectively. The final 125I solution was of high radiochemical, radionuclidic and chemical purities, besides, it showed high radioactive concentration that confirming its suitability for nuclear medicine applications and 125I brachytherapy sources preparation.

Several novel thiazolidinone and fused thiazolidinone derivatives bearing benzenesulfonamide moiety were synthesized and confirmed via spectral and elemental analyses. The newly synthesized compounds were evaluated for their cytotoxic activity on colorectal cancer cell line (Caco-2). All the synthesized compounds showed better activity than the reference standards (Doxorubicin and 5-FU). Investigation of the apoptotic activity of the most active compounds revealed that compounds 3a, 5a, 5c and 6c activate both caspase-3 and Fas-ligand in Caco-2 cell line. Compound 3a was the most active compound with caspase-3 concentration of 0.43 nmol/mL and Fas-ligand concentration of 775.2 pg/mL in treated Caco-2 cells. Compound 3a was radiolabeled with 99mTc and its biodistribution pattern was evaluated in vivo using normal Swiss Albino mice. 99mTc-compound 3a complex didn't exhibit any accumulation in any body organs except for its accumulation in the colon; target organ; where it showed 8.97 ± 1.35 %ID/g at 15min p. i. that elevated till 16.02 ± 2.43 %ID/g at 120min p. i.

The purpose of our study was to improve the delivery of a direct-acting antiviral drug, daclatasvir, to the site of action, liver tissues, using physically and biologically stable cationic bile-based vesicles. Accordingly, cationic bile-based vesicles were prepared as pro-bile-based vesicles and diethylaminoethyl dextran (DEAE-Dx)-stabilized bile-based vesicles to increase their stability without negatively affecting their hepatic affinity. The prepared bile-based vesicles were characterized for particle size, polydispersity index, ζ-potential, in vitro daclatasvir release, and ex vivo permeation using non-everted gut sac intestine. The in vivo biodistribution was experimented after oral administration utilizing the radiolabeling assay, where the liver showed the highest accumulation of the DEAE-Dx-stabilized bile-based vesicles after 4 h, reaching a value of 4.6% ID/g of the total oral administered dose of the labeled drug compared to drug solution, pro-bile-based vesicles, and cationic bile-based vesicles where the accumulation was 0.19, 1.3, and 0.31% ID/g, respectively. DEAE-Dx-stabilized bile-based vesicles increased the drug deposition into the liver about 42-fold compared to oral solution. The high physical stability and the high resistance to opsonization and clearance show that DEAE-Dx-stabilized bile-based vesicles could be efficiently applied for enhancing daclatasvir delivery to the liver after oral administration.

A new series of thiazolidinone (5a-g), thiazinone (9a-g) and dithiazepinone (9a-g) heterocycles bearing a benzenesulfonamide scaffold was synthesized. Cytotoxicity of these derivatives was assessed against MCF-7, HepG2, HCT-116 and A549 cancer cell lines and activity was compared to the known cytotoxic agents doxorubicin and 5-FU where the most active compounds displayed better to nearly similar IC50 values to the reference compounds. For assessing selectivity, the most active derivatives against MCF-7, 5b, 5c and 5e, were also assessed against the normal breast cell line MCF-10 A where they demonstrated high selective cytotoxicity to cancerous cells over that to normal cells. Further, the effect of the most active compounds 5b-e on MCF-7 and HepG2 cell cycle phase distribution was assessed and the tested sulfonamide derivatives were found to induce accumulation of cells in the

In the presented work, nano-crystalline titania (TiO2) was synthesized and evaluated as a novel chromatographic sorbent for the preparation of the medical 99Mo/99mTc generator. TiO2 was synthesized by dissolving TiCl4.6H2O with isopropyl alcohol to form a semisolid mass that was extensively dried and washed. The physicochemical parameters and surface area of the synthesized nano-crystalline TiO2 were evaluated. TiO2 was packed as a chromatographic column to study the sorption of 99Mo-polymolybdate (VI) anionic solution by dynamic equilibrium. The maximum sorption capacity of 99Mo was ~141±2mg Mo/g TiO2, thereby confirming its suitability for using low specific activity 99Mo for the preparation of 99Mo/99mTc generator. The elution performance of the prepared 99Mo/99mTc generator based on Ti-99Mo was evaluated. It showed high radiochemical purity (≥ 97% TcO4−), high radionuclidic purity (≥ 99.99%99mTc) and high chemical purity; all of these specifications show the suitability for use in nuclear medi...

Early and accurate detection of tumor assists in identifying more effective therapies. Gold nanoparticles (GNPs) were synthesized by green synthesis method using gallic acid (GA) then characterized and labeled with technetium-99m. This new platform was biologically evaluated in both normal and solid tumor bearing mice. The in-vivo study of [99mTc]Tc-gallic-GNPs via both I.V. and I.T injecton showed a high accumulation in tumor site. As a result, [99mTc]Tc-gallic-GNPs can be afforded as a potential nano-platform for tumor imaging.

The development of cancer theranostic nanomedicines is recommended to concurrently achieve and evaluate the therapeutic benefit and progress. The current work aims to develop gallic acid-gold nanoparticles (GA-Au NPs) as a theranostic probe for 99mTc-Doxorubicin (99mTc-DOX) based on the spatiotemporal release pattern induced intra-tumoral (IT) delivery. DOX-loaded GA-Au NPs were developed and identified via UV–Vis spectroscopy. The system was characterized for drug loading efficiency%, particle size, zeta potential, topography, in vitro DOX release and anti-proliferative activity against the MCF-7 cell-line. The factors influencing radiolabeling efficiency of DOX with 99mTc (DOX concentration, stannous chloride concentration, reaction time and pH) were optimized. The in vitro stability in mice serum and in vivo distribution studies in mice of 99mTc-DOX-loaded GA-Au NPs were investigated following IV and IT administration. Dox-loaded GA-Au NPs had a loading efficiency of 91%, a small particle size (≈50 nm), a promising zeta potential (−20 mV) and a sustained drug release profile at pH 5.3. GA-Au NPs exhibited increased anti-proliferative activity, with approximately a four-fold lower IC50 value (0.15 μg/ml) than free DOX. The optimized radiolabeling efficiency of 99mTc-DOX was ≈93%. It showed good physiological stability in mice serum for at least 8 h. The IT delivery of 99mTc-DOX-loaded GA-Au NPs in tumor-induced mice showed dramatic tumor accumulation. A maximum magnitude of 86.73%ID/g was achieved, at 15 min post-injection, with a target/non-target ratio of ≈56. 99mTc-DOX-loaded GA-Au NPs could be used for the selective IT delivery of a chemotherapeutic agent and an imaging agent to a target organ.

New functionalized acrylamide derivatives bearing sulfisoxazole moiety were designed to target bacterial dihydropteroate synthase (DHPS). The in vitro antimicrobial activities of these compounds were assessed. The E-configuration of compound 5b was proved by single crystal X-ray analysis. Compounds 5g and 5h displayed double the activity of ampicillin against B. subtilis. Also, 5h was two times more active than gentamycin against E. coli. Interestingly, compounds 5f-g, 7c, 8a, 8c exhibited two folds the potency of amphotericin B against S. racemosum while 5h displayed three folds the activity of amphotericin B against S. racemosum. Most of the synthesized compounds showed superior activities to the parent sulfisoxazole and were non-toxic to normal cells. DHPS is confirmed to be a putative target for our compounds via antagonizing their antibacterial activity by the folate precursor (p-aminobenzoic acid) and product (methionine) on E. coli ATCC 25922. Docking experiments against DHPS rationalized the observed antibacterial activity. Additionally, compound 5g was evaluated as a selective targeting vector for 99mTc that showed a remarkable uptake and targeting ability towards the infection site that was induced in mice.

There is an increasing interest in nanoparticles nowadays. In this review, we will enlighten the use of nanoparticles for detection and quantification of some drugs, antibiotics, antivirals, and amino acids using different analytical methods.

Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation ofThe radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 μg of SnClA newThese promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging.

BACKGROUND: The evolution of nanoparticles has gained prominence as platforms for developing diagnostic and/or therapeutic radiotracers. This study aims to develop a novel technique for fabricating a tumor diagnostic probe based on iron oxide nanoparticles excluding the utilization of chelating ligands. METHODS: Tc-99 m radionuclide was loaded into magnetic iron oxide nanoparticles platform (MIONPs) by sonication. (99m)Tc-encapsulated MIONPs were fully characterized concerning particles size, charge, radiochemical purity, encapsulation efficiency, in-vitro stability and cytotoxicity. These merits were biologically evaluated in normal and solid tumor bearing mice via different delivery approaches. RESULTS: (99m)Tc-encapsulated MIONPs probe was synthesized with average particle size 24.08 ± 7.9 nm, hydrodynamic size 52 nm, zeta potential -28 mV, radiolabeling yield 96 ± 0.83%, high in-vitro physiological stability, and appropriate cytotoxicity behavior. The in-vivo evaluation in solid tumor bearing mice revealed that the maximum tumor radioactivity accumulation (25.39 ± 0.57, 36.40 ± 0.59 and 72.61 ± 0.82%ID/g) was accomplished at 60, 60 and 30 min p.i. for intravenous, intravenous with physical magnet targeting and intratumoral delivery, respectively. The optimum T/NT ratios of 57.70, 65.00 and 87.48 were demonstrated at 60 min post I.V., I.V. with physical magnet targeting and I.T. delivery, respectively. These chemical and biological characteristics of our prepared nano-probe demonstrate highly advanced merits over the previously reported chelator mediated radiolabeled nano-formulations which reported maximum tumor uptakes in the scope of 3.65 ± 0.19 to 16.21 ± 2.56%ID/g. CONCLUSION: Stabilized encapsulation of (99m)Tc radionuclide into MIONPs elucidates a novel strategy for developing an advanced nano-sized radiopharmaceutical for tumor diagnosis. [Figure: see text]

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.

Challenges facing cardiovascular imaging necessitate innovation of better radiopharmaceuticals to augment or replace the existing ones. This research assesses the ability and competency of radioiodinated esmolol as a potential cardio selective imaging agent. Radioiodinated esmolol was synthesized with 97.3 ± 0.3% radiochemical yield and with high stability up to 48 h at room temperature as well as in rat serum. Molecular modeling study was performed to confirm the binding of iodinated esmolol to β1-adrenergic receptor. Its biodistribution studies in normal Swiss albino mice showed high heart uptake (38.5 ± 0.11%ID/g at 5 min p.i.), heart/liver ratio nearly 3.85:1 and heart/lungs ratio was about 7:1 at 5 min p.i. The evidenced selectivity of the radioiodinated esmolol to β1-adrenoceptor was confirmed by prior injection of cold esmolol. Gamma camera biodistribution pattern showed that radioiodinated esmolol accumulated selectively in heart.