Kit formulation for 99mTc-labeling of HYNIC-βAla-Bombesin(7–14)

Barros, André Luís Branco de; Mota, Luciene das Graças; Ferreira, Carolina de Aguiar; Cardoso, Valbert Nascimento

doi:10.1016/j.apradiso.2012.06.022

Cited by 19 publications

(13 citation statements)

References 33 publications

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“…The HYNIC-AF7p conjugate was prepared by coupling AF7p with HYNIC-NHS in slightly basic condition (pH 8.5) in DMF [ 24 , 25 ]. Briefly, NHS-HYNIC (216.03 μg, 0.8641 μmol) and AF7p-Dde (1.23 mg, 0.6043 μmol) were dissolved in DMF (200 μL) and DIPEA (0.43 μL, 2.63 μmol) was further added to adjust pH around 8 to 8.5.…”

Section: Methodsmentioning

confidence: 99%

Development of a Radiolabeled Peptide-Based Probe Targeting MT1-MMP for Breast Cancer Detection

Min

Zhao

et al. 2015

PLoS ONE

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Breast cancer is one of the most frequent and aggressive primary tumors among women of all races. Matrix metalloproteinase (MMPs), a family of zinc- and calcium-dependent secreted or membrane anchored endopeptidases, is overexpressed in varieties of diseases including breast cancer. Therefore, noninvasive visualization and quantification of MMP in vivo are of great interest in basic research and clinical application for breast cancer early diagnosis. Herein, we developed a 99mTc labeled membrane type I matrix metalloproteinase (MT1-MMP) specific binding peptide, [99mTc]-(HYNIC-AF7p)(tricine)(TPPTS), for in vivo detection of MDA-MB-231 breast tumor by single photon emission computed tomography (SPECT). [99mTc]-(HYNIC-AF7p)(tricine)(TPPTS) demonstrated nice biostability and high MT1-MMP binding affinity in vitro and in vivo. Tumor-to-muscle ratio was found to reach to the highest (4.17±0.49) at 2 hour after intravenously administration of [99mTc]-(HYNIC-AF7P)(tricine)(TPPTS) into MDA-MB-231 tumor bearing mice. Overall, [99mTc]-(HYNIC-AF7P)(tricine)(TPPTS) demonstrated great potential for MT1-MMP targeted detection in vivo and it would be a promising molecular imaging probe that are probably beneficial to breast cancer early diagnoses.

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Section: Methodsmentioning

confidence: 99%

Development of a Radiolabeled Peptide-Based Probe Targeting MT1-MMP for Breast Cancer Detection

Min

Zhao

et al. 2015

PLoS ONE

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“…The method for 99m Tc labeling of BIM was developed in our laboratory, based on the radiolabeling protocols developed by Nunan et al [40] and de Barros et al [41], with modifications. BIM was dissolved in 1.0 mL of phosphate buffer (pH 7.4) and radiolabeled with 99m Tc by direct labeling method using stannous chloride as reducing agent.…”

Section: Methodsmentioning

confidence: 99%

Bimatoprost-Loaded Ocular Inserts as Sustained Release Drug Delivery Systems for Glaucoma Treatment: In Vitro and In Vivo Evaluation

et al. 2014

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The purpose of the present study was to develop and assess a novel sustained-release drug delivery system of Bimatoprost (BIM). Chitosan polymeric inserts were prepared using the solvent casting method and characterized by swelling studies, infrared spectroscopy, differential scanning calorimetry, drug content, scanning electron microscopy and in vitro drug release. Biodistribution of 99mTc-BIM eye drops and 99mTc-BIM-loaded inserts, after ocular administration in Wistar rats, was accessed by ex vivo radiation counting. The inserts were evaluated for their therapeutic efficacy in glaucomatous Wistar rats. Glaucoma was induced by weekly intracameral injection of hyaluronic acid. BIM-loaded inserts (equivalent to 9.0 µg BIM) were administered once into conjunctival sac, after ocular hypertension confirmation. BIM eye drop was topically instilled in a second group of glaucomatous rats for 15 days days, while placebo inserts were administered once in a third group. An untreated glaucomatous group was used as control. Intraocular pressure (IOP) was monitored for four consecutive weeks after treatment began. At the end of the experiment, retinal ganglion cells and optic nerve head cupping were evaluated in the histological eye sections. Characterization results revealed that the drug physically interacted, but did not chemically react with the polymeric matrix. Inserts sustainedly released BIM in vitro during 8 hours. Biodistribution studies showed that the amount of 99mTc-BIM that remained in the eye was significantly lower after eye drop instillation than after chitosan insert implantation. BIM-loaded inserts lowered IOP for 4 weeks, after one application, while IOP values remained significantly high for the placebo and untreated groups. Eye drops were only effective during the daily treatment period. IOP results were reflected in RGC counting and optic nerve head cupping damage. BIM-loaded inserts provided sustained release of BIM and seem to be a promising system for glaucoma management.

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“…TLC is an important method to evaluate radiochemical yield of labeled compounds, since it is a fast, reliable and easy test to perform. The presence of radiochemical impurities proved to be a drawback in nuclear medicine, yielding images in poor quality [20]. Thus, it can be concluded that radiopharmaceuticals should be efficiently radiolabeled (above 90%).…”

Section: Radiochemical Yieldsmentioning

confidence: 98%

Synthesis, characterization, and biodistribution studies of 99m Tc-labeled SBA-16 mesoporous silica nanoparticles

Barros

Ferraz

Dantas

et al. 2015

Materials Science and Engineering: C

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Kit formulation for 99mTc-labeling of HYNIC-βAla-Bombesin(7–14)

Cited by 19 publications

References 33 publications

Development of a Radiolabeled Peptide-Based Probe Targeting MT1-MMP for Breast Cancer Detection

Development of a Radiolabeled Peptide-Based Probe Targeting MT1-MMP for Breast Cancer Detection

Bimatoprost-Loaded Ocular Inserts as Sustained Release Drug Delivery Systems for Glaucoma Treatment: In Vitro and In Vivo Evaluation

Synthesis, characterization, and biodistribution studies of 99m Tc-labeled SBA-16 mesoporous silica nanoparticles

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