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1.
Eur J Pharm Sci ; 122: 239-245, 2018 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-29981892

RESUMO

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 ±â€¯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 ±â€¯1.12 and 63.8 ±â€¯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 ±â€¯0.65 and 92.46 ±â€¯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.


Assuntos
Sistemas de Liberação de Medicamentos , Radioisótopos do Iodo/administração & dosagem , Nanopartículas Metálicas/administração & dosagem , Sarcoma/diagnóstico , Sarcoma/tratamento farmacológico , Prata/administração & dosagem , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Humanos , Radioisótopos do Iodo/química , Radioisótopos do Iodo/farmacocinética , Radioisótopos do Iodo/uso terapêutico , Masculino , Nanopartículas Metálicas/química , Nanopartículas Metálicas/uso terapêutico , Camundongos , Sarcoma/metabolismo , Prata/química , Prata/farmacocinética , Prata/uso terapêutico , Nanomedicina Teranóstica , Distribuição Tecidual
2.
Appl Radiat Isot ; 115: 37-44, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27337647

RESUMO

Clomiphene has growth-inhibitory effects of breast cancer cells, clomiphene was successfully labeled with (125)I via direct electrophilic substitution reaction with labeling yield 97%. It was obtained at optimum substrate amount of 0.5mg, Chloramine-T was used as an oxidizing agent at optimum amount of 25µg. Labeling reactions was done at pH 5 at ambient temperature. This study showed good in vitro and in vivo stability of the (125)I-clomiphene. The radiolabeled compound showed high ascetic fluid uptake of 18.12±0.27% at 30min post-injection. Solid tumor uptake of (125)I-clomiphene was 12.48±0.32% at 30min post-injection. This data revealed the localization of tracer in tumor tissue with high percent sufficient to use (125)I-clomiphene as a promising tool for the diagnosis of breast cancer.


Assuntos
Neoplasias da Mama/diagnóstico por imagem , Clomifeno/farmacocinética , Antagonistas de Estrogênios/farmacocinética , Linhagem Celular Tumoral , Cloraminas , Humanos , Marcação por Isótopo , Distribuição Tecidual , Compostos de Tosil
3.
J Labelled Comp Radiopharm ; 57(10): 593-9, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25196119

RESUMO

Acebutolol was successfully labeled with (125) I via direct electrophilic substitution reaction. Radioiodinated acebutolol was prepared with a maximum radiochemical yield of 96.5 ± 0.3% and in vitro stability up to 72 h. The in vivo biological distribution of radioiodinated acebutolol showed high heart uptake of 37.8 ± 0.14% injected activity/g organ with low lungs and liver uptakes at 5 min post-injection. In vivo receptor blocking study was carried out in mice to evaluate its selectivity to heart. Radioiodinated acebutolol showed fast heart accumulation with high heart/liver ratio, which provides the ability for fast myocardial imaging with significant decrease in the radiation hazards risk on patients. So, radioiodinated acebutolol could be displayed as a radiotracer drug of choice in case of emergency patients for myocardial perfusion imaging.


Assuntos
Acebutolol/farmacocinética , Imagem de Perfusão do Miocárdio/métodos , Compostos Radiofarmacêuticos/farmacocinética , Acebutolol/síntese química , Animais , Radioisótopos do Iodo/química , Radioisótopos do Iodo/farmacocinética , Masculino , Camundongos , Compostos Radiofarmacêuticos/síntese química , Distribuição Tecidual
4.
Hum Antibodies ; 16(3-4): 67-71, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-18334742

RESUMO

This paper addresses the production of effective luteinizing hormone antisera by two different immunization methods; the traditional and modified methods. The main difference between these two methods is in the immunization procedure. In the modified method, an additional injection of emulsion with complete Freund's adjuvant and only one booster are applied at the third and 28th day from the first injection, respectively. The results of the study indicated the possibility of producing the antiseria using the modified method in short time and better quality than those produced by the traditional methods. The details of both methods are presented together with the results obtained from the antibodies detection. Comparison between these two methods is also presented along with discussions.


Assuntos
Soros Imunes/biossíntese , Hormônio Luteinizante/imunologia , Animais , Afinidade de Anticorpos , Reações Cruzadas , Soros Imunes/imunologia , Imunização , Masculino , Coelhos
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