Novel rivaroxaban-loaded poly(lactic-co-glycolic acid)/poloxamer nanoparticles: preparation, physicochemical characterization, in vitro evaluation of time-dependent anticoagulant activity and toxicological profile
| Autor: | Plínio Cunha Sathler, Lucio Mendes Cabral, Alice Simon, Marcela Cristina de Moraes, Cristina da Costa Bernardes Araújo, Flávia Almada do Carmo, Priscila de Souza Furtado, Monique Etnea Machado, Luiz Cláudio Rodrigues Pereira da Silva |
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| Rok vydání: | 2020 |
| Předmět: |
Drug
Materials science medicine.drug_mechanism_of_action Cell Survival media_common.quotation_subject Factor Xa Inhibitor Bioengineering 02 engineering and technology Poloxamer Pharmacology 010402 general chemistry 01 natural sciences Hemolysis chemistry.chemical_compound Pharmacokinetics Polylactic Acid-Polyglycolic Acid Copolymer Rivaroxaban Chlorocebus aethiops medicine Animals Humans General Materials Science Electrical and Electronic Engineering Particle Size Vero Cells Glycolic acid media_common Drug Carriers Mechanical Engineering Anticoagulants General Chemistry 021001 nanoscience & nanotechnology medicine.disease 0104 chemical sciences Rats PLGA Drug Liberation chemistry Mechanics of Materials Nanoparticles 0210 nano-technology medicine.drug Factor Xa Inhibitors |
| Zdroj: | Nanotechnology. 32(13) |
| ISSN: | 1361-6528 |
| Popis: | Rivaroxaban (RXB), an oral direct factor Xa inhibitor, presents innovative therapeutic profile. However, RXB has shown adverse effects, mainly due to pharmacokinetic limitations, highlighting the importance of developing more effective formulations. Therefore, this work aims at the preparation, physicochemical characterization and in vitro evaluation of time-dependent anticoagulant activity and toxicology profile of RXB-loaded poly(lactic-co-glycolic acid) (PLGA)/poloxamer nanoparticles (RXBNps). RXBNp were produced by nanoprecipitation method and physicochemical characteristics were evaluated. In vitro analysis of time-dependent anticoagulant activity was performed by prothrombin time test and toxicological profile was assessed by hemolysis and MTT reduction assays. The developed RXBNp present spherical morphology with average diameter of 205.5 ± 16.95 nm (PdI 0.096 ± 0.04), negative zeta potential (−26.28 ± 0.77 mV), entrapment efficiency of 91.35 ± 2.40%, yield of 41.81 ± 1.68% and 3.72 ± 0.07% of drug loading. Drug release was characterized by an initial fast release followed by a sustained release with 28.34 ± 2.82% of RXB available in 72 h. RXBNp showed an expressive time-dependent anticoagulant activity in human and rat blood plasma and non-toxic profile. Based on the results presented, it is possible to consider that RXBNp may be able to assist in the development of promising new therapies for treatment of thrombotic disorders. |
| Databáze: | OpenAIRE |
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