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Biomed Pharmacother ; 107: 1259-1267, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30257340

RESUMO

Meloxicam is an anti-inflammatory drug that has a potential protective effect in many common diseases. However, this molecule is quickly eliminated from the body due to it short half-life. One way to overcome this problem is to incorporate meloxicam into lipid-core nanocapsules which may increase it anti-inflammatory effects. In view of this, the objective of this work was to evaluate the potential toxicity and safety of these novel nanomaterials both in vitro and in vivo. Here, we evaluated the effects of uncoated meloxicam-loaded nanocapsules (M-NC), uncoated and not loaded with meloxicam or blank (B-NC), PEGylated meloxicam-loaded lipid-core nanocapsules (M-NCPEG), blank PEGylated lipid-core nanocapsules (B-NCPEG) and free meloxicam (M-F) in vitro through the analysis of cell viability, caspase activity assays and gene expression of perforin and granzyme B. Meanwhile, the in vivo safety was assessed using C57BL/6 mice that received nanocapsules for seven days. Thus, no change in cell viability was observed after treatments. Furthermore, M-NC, M-NCPEG and M-F groups reversed the damage caused by H2O2 on caspase-1, 3 and 8 activities. Overall, in vivo results showed a safe profile of these nanocapsules including hematological, biochemical, histological and genotoxicity analysis. In conclusion, we observed that meloxicam nanocapsules present a safe profile to use in future studies with this experimental protocol and partially reverse in vitro damage caused by H2O2.


Assuntos
Anti-Inflamatórios não Esteroides , Caspases/metabolismo , Linfócitos/efeitos dos fármacos , Meloxicam , Nanocápsulas/química , Polietilenoglicóis/química , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/toxicidade , Peso Corporal/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Dano ao DNA , Ingestão de Alimentos/efeitos dos fármacos , Humanos , Peróxido de Hidrogênio/toxicidade , Linfócitos/enzimologia , Linfócitos/patologia , Masculino , Meloxicam/farmacologia , Meloxicam/toxicidade , Camundongos , Camundongos Endogâmicos C57BL , Especificidade de Órgãos , Baço/efeitos dos fármacos , Baço/patologia , Testes de Toxicidade
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