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AAPS PharmSciTech ; 25(6): 145, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38918292

RESUMO

The objective of the current research was to develop abietic acid (AA)-loaded hybrid polymeric nanoparticles (HNPs) for anti-inflammatory and antioxidant activity after oral administration. AAHNPs were developed by microinjection technique and optimized by 3-factor 3-level Box-Behnken design. The AAHNPs were evaluated for morphology, FTIR, X-ray diffraction, in-vitro release, ex-vivo permeation, in-vitro antioxidant, and in-vivo anti-inflammatory activity. The optimized AAHNPs (AAHNPsopt) displayed 384.5 ± 6.36nm of PS, 0.376 of PDI, 23.0 mV of ZP, and 80.01 ± 1.89% of EE. FTIR and X-ray diffraction study results revealed that AA was encapsulated into a HNPs matrix. The AAHNPsopt showed significant (P < 0.05) high and sustained release of AA (86.72 ± 4.92%) than pure AA (29.87 ± 3.11%) in 24h. AAHNPsopt showed an initial fast release of AA (20.12 ± 3.07% in 2h), which succeeded in reaching the therapeutic concentration. The AAHNPsopt showed 2.49-fold higher ex-vivo gut permeation flux than pure AA due to the presence of lipid and surfactant. The AAHNPsopt exhibited significantly (P < 0.05, P < 0.01, P < 0.001) higher antioxidant activity as compared to pure AA at each concentration. AAHNPsopt formulation displayed a significantly (P < 0.05) higher anti-inflammatory effect (21.51 ± 2.23% swelling) as compared to pure AA (46.51 ± 1.74% swelling). From the in-vitro and in-vivo finding, it was concluded that HNPs might be a suitable carrier for the improvement of the therapeutic efficacy of the drug.


Assuntos
Abietanos , Anti-Inflamatórios , Antioxidantes , Portadores de Fármacos , Lipídeos , Nanopartículas , Polímeros , Nanopartículas/química , Animais , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/administração & dosagem , Antioxidantes/farmacocinética , Ratos , Polímeros/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacocinética , Lipídeos/química , Portadores de Fármacos/química , Abietanos/farmacologia , Abietanos/administração & dosagem , Abietanos/química , Difração de Raios X/métodos , Liberação Controlada de Fármacos , Administração Oral , Masculino , Tamanho da Partícula , Ratos Wistar , Química Farmacêutica/métodos
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