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Un enfoque pro-droga versátil para la carga del núcleo liposomal de los fármacos anticancerígenos de la camptotecina
Xinli Liu1, Bert C Lynn, Junhong Zhang
1Department of Chemistry and Pharmaceutical Sciences, Markey Cancer Center, University of Kentucky, Lexington, KY 40506, USA.
Journal of the American Chemical Society
|June 27, 2002
Resumen
Una nueva estrategia de prodrogas permite la carga liposomal de camptotecinas insolubles en agua. Este enfoque facilita la orientación del tumor y la liberación controlada de camptotecina activa en el sitio del tumor.
Área de la Ciencia:
- Química Farmacéutica Química Farmacéutica es el campo de la química farmacéutica.
- Sistemas de suministro de drogas Sistemas de suministro de drogas.
- Nanotecnología La nanotecnología es la nanotecnología.
Sus antecedentes:
- Las camptotecinas son potentes agentes anticancerígenos con poca solubilidad en agua, lo que limita su aplicación clínica.
- Las formulaciones liposomales ofrecen una estrategia para mejorar la solubilidad y la administración de fármacos.
- La carga eficiente de medicamentos insolubles en agua en los liposomas sigue siendo un desafío.
Objetivo del estudio:
- Desarrollar una estrategia pro-droga versátil para cargar eficazmente las camptotecinas insolubles en agua en los liposomas.
- Para crear un sistema prodrug que facilita la liberación del fármaco activo en el sitio del tumor.
- Para permitir la administración dirigida al tumor de análogos lipofílicos de la camptotecina.
Principales métodos:
- Conversión de los análogos activos de la camptotecina a los precursores de los ésteres omega-aminoalcanoicos.
- Utilizando el grupo amino del prodrug para mejorar la solubilidad en agua y la capacidad de respuesta a los gradientes de sulfato de amonio para la carga liposomal.
- Diseñar el prodrogo para la descomposición no enzimática y la liberación activa del fármaco a pH fisiológico.
Principales resultados:
- La estrategia de prodrogación facilitó con éxito la carga activa de camptotecinas en el núcleo acuoso liposomal.
- El prodrogo se somete a ciclización y rápida descomposición no enzimática a pH fisiológico (≥7), liberando camptotecina activa.
- La velocidad de formación del agente activo se puede modular alterando la longitud del espaciador de alquilo (n).
Conclusiones:
- Esta nueva estrategia de pródrogas liposomales proporciona un sistema versátil para administrar camptotecinas insolubles en agua, incluidas la SN-38, la 9-nitrocamptotecina y la DB-67.
- El enfoque ofrece potencial para la terapia tumoral dirigida con cinética de liberación de fármacos controlables.
- Este método supera las limitaciones asociadas con la escasa solubilidad de los análogos de la camptotecina.
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