Informace o publikaci

Polymer nanotherapeutics with the controlled release of acetylsalicylic acid and its derivatives inhibiting cyclooxygenase isoforms and reducing the production of pro-inflammatory mediators

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FREJKOVÁ Markéta BĚHALOVÁ Kateřina RUBANOVÁ Daniela DE SANCTIS Juan Bautista KUBALA Lukáš CHYTIL Petr ŠIMONOVÁ Alice KŘÍŽEK Tomáš RANDÁROVÁ Eva GUNÁR Kristýna ETRYCH Tomáš

Rok publikování 2024
Druh Článek v odborném periodiku
Časopis / Zdroj International Journal of Pharmaceutics
Fakulta / Pracoviště MU

Přírodovědecká fakulta

Citace
www https://www.sciencedirect.com/science/article/pii/S0378517324009761
Doi http://dx.doi.org/10.1016/j.ijpharm.2024.124742
Klíčová slova Drug delivery; HPMA; Nanotherapeutics; Inflammation; Acetylsalicylic acid; Salicylic acid hydrazide
Popis The effective treatment of inflammatory diseases, particularly their chronic forms, is a key task of modern medicine. Herein, we report the synthesis and evaluation of biocompatible polymer conjugates based on N-2(hydroxypropyl)methacrylamide copolymers enabling the controlled release of acetylsalicylic acid (ASA)-based anti-inflammatory drugs under specific stimuli. All polymer nanotherapeutics were proposed as water-soluble drug delivery systems with a hydrodynamic size below 10 nm ensuring suitability for the parenteral application and preventing opsonization by the reticuloendothelial system. The nanotherapeutics bearing an esterbound ASA exhibited long-term release of the ASA/salicylic acid mixture, while the nanotherapeutics carrying salicylic acid hydrazide (SAH) ensured the selective release of SAH in the acidic inflammatory environment thanks to the pH-sensitive hydrazone bond between the polymer carrier and SAH. The ASA- and SAH-containing nanotherapeutics inhibited both cyclooxygenase isoforms and/or the production of pro-inflammatory mediators. Thanks to their favorable design, they can preferentially accumulate in the inflamed tissue, resulting in reduced side effects and lower dosage, and thus more effective and safer treatment.

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