Sulforaphane-loaded hyaluronic acid-poloxamer hybrid hydrogel enhances cartilage protection in osteoarthritis models

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2021
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Materials Science & Engineering C
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Sulforaphane (SFN) is an isothiocyanate with anti-arthritic and immuno-regulatory activities, supported by the downregulation of NF-κB pathway, reduction on metalloproteinases expression and prevention of cytokine-induced cartilage degeneration implicated in OA progression. SFN promising pharmacological effects associated to its possible use, by intra-articular route and directly in contact to the site of action, highlight SFN as promising candidate for the development of drug-delivery systems. The association of poloxamers (PL) and hyaluronic acid (HA) supports the development of osteotrophic and chondroprotective pharmaceutical formulations. This study aims to develop PL-HA hybrid hydrogels as delivery systems for SFN intra-articular release and evaluate their biocompatibility and efficacy for osteoarthritis treatment. All formulations showed viscoelastic behavior and cubic phase organization. SFN incorporation and drug loading showed a concentration-dependent behavior following HA addition. Drug release profiles were influenced by both diffusion and relaxation of polymeric chains mechanisms. The PL407-PL338-HA-SFN hydrogel did not evoke pronounced cytotoxic effects on either osteoblast or chondrosarcoma cell lines. In vitro/ex vivo pharmacological evaluation interfered with an elevated activation of NF-κB and COX-2, increased the type II collagen expression, and inhibited proteoglycan depletion. These results highlight the biocompatibility and the pharmacological efficacy of PL-HA hybrid hydrogels as delivery systems for SFN intra-articular release for OA treatment.

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NASCIMENTO, MONICA H.M. do; AMBROSIO, FELIPE N.; FERRARAZ, DEBORA C.; WINDISCH-NETO, HERMANN; QUEROBINO, SAMYR M.; NASCIMENTO-SALES, MICHELLE; ALBERTO-SILVA, CARLOS; CHRISTOFFOLETE, MARCELO A.; FRANCO, MARGARETH K.K.D.; KENT, BEN; YOKAICHIYA, FABIANO; LOMBELLO, CHRISTIANE B.; ARAUJO, DANIELE R. de. Sulforaphane-loaded hyaluronic acid-poloxamer hybrid hydrogel enhances cartilage protection in osteoarthritis models. Materials Science & Engineering C, v. 128, p. 1-15, 2021. DOI: 10.1016/j.msec.2021.112345. Disponível em: http://repositorio.ipen.br/handle/123456789/32362. Acesso em: 19 Apr 2024.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.

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