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Inicio Revista Española de Medicina Nuclear e Imagen Molecular (English Edition) Technetium-99m-labeled lapachol as an imaging probe for breast tumor identificat...
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Vol. 38. Issue 3.
Pages 167-172 (May - June 2019)
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Vol. 38. Issue 3.
Pages 167-172 (May - June 2019)
Original Article
Technetium-99m-labeled lapachol as an imaging probe for breast tumor identification
Lapachol marcado con tecnecio 99m como sonda de imágenes para la identificación de tumores de mama
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Sued E.M. Mirandaa, Janaína A. Lemosa, Renata S. Fernandesb, Flaviano Melo Ottonib, Ricardo J. Alvesb, Alice Ferrettic, Domenico Rubelloc,
Corresponding author
domenico.rubello@libero.it

Corresponding authors.
, Valbert N. Cardosoa, André L.B. de Barrosa,
Corresponding author
a Department of Clinical and Toxicological Analysis, Faculty of Pharmacy, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Minas Gerais, Brazil
b Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Minas Gerais, Brazil
c Department of Nuclear Medicine, Radiology, NeuroRadiology, Medical Physics, Clinical Laboratory, Microbiology, Pathology, Santa Maria della Misericordia Hospital, Rovigo, Italy
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Abstract
Aim

Breast cancer is a health problem worldwide with high incidence and mortality rates. It is well known that the development of more sensitive and specific diagnostic methods is of great importance since an early diagnosis is essential to successfully treat tumors. Lapachol is a natural compound, belonging to the naphthoquinone group that has been widely used in traditional medicine to treat various illnesses, including cancer. The aim of this study was to evaluate technetium-99m-labeled lapachol as an imaging probe for breast cancer identification.

Methods

To achieve this purpose, lapachol was labeled with technetium-99m, radiochemical purity and in vitro stability were determined. Blood clearance, in healthy mice, and biodistribution, in 4T1 tumor-bearing mice, were also evaluated.

Results

Lapachol was successfully labeled with technetium-99m, with high values of radiochemical yield (95.9±3.4%). In vitro stability showed that the radiolabeled complex remained stable for up to 24h, with values above 90% for both saline and plasma (95.6±3.6% and 96.4±1.7%, respectively). The radiolabeled complex decays in a biphasic manner, with a half-life of distribution and elimination equal to 3.3 and 50.0min, respectively. Biodistribution and scintigraphic images showed high uptake in organs of excretion (kidneys, liver, and intestine). It could be also noted that tumor uptake was higher than the muscle at all time points. Tumor-to-muscle ratio reaches ∼4.5 at 24h after administration.

Conclusion

These findings suggest that 99mTc-Lapachol can be a potential diagnostic agent for breast tumors.

Keywords:
Lapachol
Tumor
Technetium-99m
Diagnosis
Radiopharmaceutical
Resumen
Objetivo

El cáncer de mama es un problema de salud en todo el mundo con altas tasas de incidencia y mortalidad. Es bien sabido que el desarrollo de métodos de diagnóstico más sensibles y específicos es de gran importancia, ya que un diagnóstico precoz es esencial para tratar con éxito los tumores. Lapachol es un compuesto natural, perteneciente al grupo de la naftoquinona, que se ha utilizado ampliamente en la medicina tradicional para tratar diversas enfermedades, incluido el cáncer. El objetivo de este estudio fue evaluar el lapachol marcado con tecnecio 99m como una sonda de imágenes para la identificación del cáncer de mama.

Métodos

Para lograr este propósito, el lapachol se marcó con tecnecio-99m, se determinó la pureza radioquímica y la estabilidad in vitro. También se evaluó el aclaramiento en sangre en ratones sanos y la biodistribución en ratones con tumor 4T1.

Resultados

Lapachol fue exitosamente marcado con tecnecio-99m, con altos valores de rendimiento radioquímico (95.9±3.4%). La estabilidad in vitro mostró que el complejo radiomarcado permaneció estable durante hasta 24h, con valores superiores al 90% tanto para solución salina como para plasma (95,6±3,6% y 96,4±1,7%, respectivamente). El complejo radiomarcado decae de forma bifásica, con una vida media de distribución y eliminación igual a 3.3 y 50.0min, respectivamente. La biodistribución y las imágenes gammagráficas mostraron una alta captación en los órganos de excreción (riñones, hígado e intestino). También se puede observar que la captación tumoral fue mayor que en el músculo en todos los puntos temporales. La relación de tumor / músculo alcanza ∼ 4.5 a las 24h después de la administración.

Conclusión

Estos hallazgos sugieren que 99mTc-Lapachol puede ser un potencial agente de diagnóstico para los tumores de mama.

Palabras clave:
Lapachol
Tumor
Tecnecio-99m
Diagnóstico
Radiofármaco

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