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Terapia para el dolor
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Terapia para el dolor

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Científicos del Hospital Infantil de Boston y la Facultad de Medicina de Harvard (EEUU) han ideado una forma para administrar anestésicos locales y aliviar el dolor durante periodos de más de 48 horas. Lo más sorprendente de este experimento, descrito en las páginas de 'Proceedings of the National Academy os Sciences' ('PNAS'), es que en la mayor parte de los casos no se produjo toxicidad, el problema más común de la analgesia a largo plazo.

Aún no se ha probado en humanos pero sus diseñadores están muy esperanzados por los resultados obtenidos en ratones. Daniel Kohane, especialista en anestesiología en las citadas instituciones, y sus colegas decidieron abordar el tema de la analgesia de larga duración. Hasta la fecha, se han puesto a prueba numerosas técnicas pero, a pesar de que muchos han logrado prolongar el alivio del dolor, siempre se presentaba el problema de la toxicidad, que limitaba su uso.

"La idea era que una única inyección pudiera producir un bloqueo nervioso [que alivia el dolor] que durara días, semanas, tal vez meses", ha explicado Kohane. Para ello, fijaron su atención en un tipo de compuestos bloqueadores específicos de los canales de sodio capaces de producir una gran anestesia sin ser apenas tóxicos. El inconveniente: que al ser muy hidrófilos (afines al agua) son difíciles de encapsular. Además, los materiales utilizados normalmente para envolver estos fármacos producían daño celular por sí mismos.

Para salvar estos obstáculos, desarrollaron liposomas, pequeñas vesículas con una doble membrana compuesta de lípidos, de dos clases: fluidos y sólidos. En ellos introdujeron los fármacos. El STX, uno de estos bloqueadores de canales de sodio, bupivacaína (otro anestésico local) y/o dexametasona (potente antiinflamatorio). Las inyecciones se practicaron en el nervio ciático de varios roedores.

Buenos resultados
El bloqueo nervioso empezó 10-15 minutos después del pinchazo con los liposomas fluidos y 60-90 minutos después con los sólidos. La mayor parte de los ratones no experimentó toxicidad alguna, salvo una reacción inflamatoria local que se resolvió de forma espontánea. Sólo en el caso de liposomas rellenos con STX y altas concentraciones de dexametasona se produjo una reacción adversa muy fuerte.

La duración de la analgesia varió en función del tipo de liposoma y del fármaco que contenía pero los tiempos iban desde algo más de siete horas (con la bupivacaína) hasta los dos días de anestesia que experimentaron los roedores inyectados con STX en liposomas sólidos. Resultados que "suponen una gran mejoría" respecto a estudios anteriores, explican los autores en las páginas de 'PNAS'.

Otras pruebas de laboratorio confirmaron que el STX no es tóxico para el músculo ni para el sistema nervioso y un análisis de la expresión de cuatro genes relacionados con el daño de los nervios ratificó esto último en los ratones.

Aunque quedan muchas cosas por hacer, "si estas fórmulas de anestésicos locales de baja toxicidad y efecto de larga duración muestran ser eficaces en humanos, podrían tener un gran impacto sobre el tratamiento del dolor agudo y crónico", ha explicado Alison Cole, del Instituto Nacional de Ciencias Médicas Generales, que ha financiado parcialmente el proyecto.

Michael Chorny y Robert Levy, del Hospital Infantil de Filadelfia (EEUU), analizan en un artículo las consecuencias de los experimentos de Kohane y sus colegas, que califican de "avance único y prometedor para la analgesia específica". Además de su posible uso para tratar el dolor crónico localizado que no responde a otras terapias o la anestesia intraarticular, la aplicación de estos liposomas podría ser útil también para la distribución de otro tipo de fármacos.

"Los liposomas, capaces de contener tanto sustancias solubles en agua como lipofílicas [...] y con un historial de seguridad en su uso clínico presentan, obviamente, una ventaja", señalan Chorny y Levy. elmundosalud
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