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Entrega biológica mediada por boronato.

Gregory A Ellis1, Michael J Palte, Ronald T Raines

  • 1Department of Biochemistry, University of Wisconsin-Madison, Madison, Wisconsin 53706, USA.

Journal of the American Chemical Society
|February 7, 2012
PubMed
Resumen
Este resumen es generado por máquina.

Los ácidos borónicos pueden mejorar la administración de fármacos grandes a las células al interactuar con los azúcares de la superficie celular. Este nuevo enfoque ofrece un método no dañino para mejorar la administración de fármacos macromoleculares a las células de mamíferos.

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Área de la Ciencia:

  • La bioquímica es la bioquímica.
  • Biología celular Biología celular.
  • Entrega de drogas Envío de drogas

Sus antecedentes:

  • La administración de fármacos macromoleculares a las células se ve obstaculizada por mecanismos de captación celular ineficientes.
  • Las superficies celulares son ricas en sacarídeos, que presentan objetivos potenciales para los portadores de fármacos.
  • Se sabe que los ácidos borónicos forman enlaces covalentes reversibles con los diolos que se encuentran en los sacáridos.

Objetivo del estudio:

  • Investigar el potencial de los ácidos borónicos como portadores para mejorar la administración citosólica de fármacos macromoleculares.
  • Demostrar una estrategia no catiónica para mejorar la entrada celular de macromoléculas polares.

Principales métodos:

  • Conjugando ácidos borónicos colgantes con una toxina proteica.
  • Evaluación de la captación celular y la eficiencia de la entrega citosólica de la toxina proteica modificada en células de mamíferos.
  • Utilizando la interacción entre los ácidos borónicos y los sacáridos de la superficie celular para una administración dirigida.

Principales resultados:

  • Los ácidos borónicos colgantes mejoraron significativamente la entrega citosólica de la toxina proteica.
  • La formación de ésteres de boronato con sacarídeos de la superficie celular facilitó la entrada celular.
  • Este método demostró ser eficaz para la entrega de una macromolécula polar en las células de mamíferos.

Conclusiones:

  • Los ácidos borónicos sirven como portadores no catiónicos efectivos para la administración de fármacos macromoleculares.
  • La interacción con los sacarídeos de la superficie celular es una estrategia viable para mejorar la internalización de fármacos.
  • Este enfoque amplía las posibilidades de suministrar moléculas terapéuticas grandes y polares en las células.