Enoxaparin is an anticoagulant widely used in the treatment and prophylaxis of deep vein thrombosis (DVT). The subcutaneous route of administration, sometimes in repeated doses during 24 hours, represents a limitation to its use. Thus, the development of a product that can be administered either subcutaneously, in a smaller number of applications becomes a major challenge, with interesting clinical applications. The use of a system for sustained release of drugs can help to meet that goal, by protecting and enabling a gradual released of the agent. This study consisted of the evaluation of in vivo anticoagulant and antithrombotic activity of biodegradable nanoparticles of poly (ε-caprolactone) (PCL) with enoxaparin after subcutaneous injection. The nanoparticles were prepared by the method of double emulsion (w/o/w) and solvent evaporation. Subcutaneous enoxaparin encapsulated in PCL nanoparticles (1000 IU/kg) showed a sustained release in vivo for up to 12 hours (Cmax 0.62 IU/mL) a significantly longer period (P < 0.01) when compared to free enoxaparin (1000 IU/Kg) that disappeared after 9 hours (Cmax 1.50 IU/mL), however with lower anti-Xa activity. The antithrombotic action of enoxaparin-nanoparticles was tested in a DVT model by stasis in rats. There were virtually no formation of venous thrombosis in any of the rats that received enoxaparin encapsulated in nanoparticles (0.03 mg), with a significant difference when compared to groups that received saline (17.2 mg, P < 0.001) and free enoxaparin (2.87 mg, P = 0.001). In summary, enoxaparin-encapsulated in polymeric nanoparticles showed a sustained release for a greater period than that of enoxaparin, and with excellent antithrombotic action. These results corroborate the promising use of pharmacological nanoparticles in clinical practice.
Título em inglês : Preparation and characterization of heparin-loaded nanoparticles and its evaluation in animal model of venous thrombosis Keywords: • Heparin • Nanoparticles iv v DEDICATÓRIA Aos meus pais, Francismar e Elisete, meus maiores exemplos de vida, amor, sabedoria e determinação. Por acreditarem nos meus sonhos e terem sido minhas asas, mais uma vez, para que eu pudesse embarcar em mais esta viagem. vi AGRADECIMENTOS A Deus, por me acompanhar por onde é que eu esteja me dando força, coragem e confiança de que sempre posso alcançar meus sonhos. A Dra. Joyce M. Annichino-Bizzachi, pelo exemplo de conduta e orientação nos aspectos científicos e profissionais de minha carreira. Ao Prof. Dr. Nelson Durán e à Dra. Priscyla Marcato pela colaboração e ensinamentos, fundamentais no desenvolvimento deste estudo, além da confiança, amizade, dedicação e paciência. A Profa. Dra. Nelci Fenalti Höehr, pelo carinho e incentivo na minha carreira acadêmica.Aos funcionários e amigos do Laboratório de Biologia Molecular em Hemostasia, Ucha, Deva e Cris, pela colaboração, amizade e paciência.Aos funcionários e amigos do Laboratório de Hemostasia, Tânia, Silmara, Susan e Ricardo, pela colaboração, paciência e amizade.
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