Diclofenac Loaded Biodegradable Nanoparticles as Antitumoral and Antiangiogenic Therapy

载双氯芬酸的可生物降解纳米粒子作为抗肿瘤和抗血管生成疗法

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作者:Gerard Esteruelas, Eliana B Souto, Marta Espina, María Luisa García, Marta Świtalska, Joanna Wietrzyk, Anna Gliszczyńska, Elena Sánchez-López

Abstract

Cancer is identified as one of the main causes of death worldwide, and an effective treatment that can reduce/eliminate serious adverse effects is still an unmet medical need. Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), has demonstrated promising antitumoral properties. However, the prolonged use of this NSAID poses several adverse effects. These can be overcome by the use of suitable delivery systems that are able to provide a controlled delivery of the payload. In this study, Diclofenac was incorporated into biodegradable polymeric nanoparticles based on PLGA and the formulation was optimized using a factorial design approach. A monodisperse nanoparticle population was obtained with a mean size of ca. 150 nm and negative surface charge. The release profile of diclofenac from the optimal formulation followed a prolonged release kinetics. Diclofenac nanoparticles demonstrated antitumoral and antiangiogenic properties without causing cytotoxicity to non-tumoral cells, and can be pointed out as a safe, promising and innovative nanoparticle-based formulation with potential antitumoral effects.

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