RESUMO
This study aimed to develop a novel ureasil-polyether transdermal hybrid matrix (U-PEO) loaded with Annona muricata concentrated extract (AMCE), which exhibits potent anti-inflammatory activity. The extract was obtained by maceration, a method that allowed for the extraction of a high concentration of flavonoids (39.27 mg/g of extract). In vivo tests demonstrated that 10 mg/kg of AMCE inhibited inflammation for 6 h. The physicochemical characterization of U-PEO with AMCE was conducted via a thermogravimetric analysis (TGA), while its surface was recorded using atomic force microscopy (AFM). The in vitro macroscopic swelling and release tests demonstrated the hydrophilic profile of the material and the percentage of AMCE released. The TGA results demonstrated that the system exhibited physical compatibility due to the thermal stability of U-PEO. Additionally, the AFM analysis revealed a rough and porous surface, with a particular emphasis on the system with AMCE. The release resulted in the liberation of 23.72% of AMCE within 24 h. Finally, the preclinical tests demonstrated that U-PEO with AMCE was also capable of effectively inhibiting inflammation for 6 h, a duration comparable to that of a commercial formulation. The results permit the advancement of the study towards the development of a transdermal system, thereby rendering its application in clinical studies feasible.
RESUMO
The crude ethanol extract (EEOH) of the bark of Maytenus rigida Mart (Celastraceae) a plant used in Brazil herbal traditional medicine, was tested for anti-inflammatory, antiulcer and antidiarrhoeal activities in animal models. No acute toxicological sign was observed in animals treated with the highest dose (5000 mg/kg, p.o. or 2000 mg/kg i.p.) of EEOH. The extract doses of 250, 500 or 750 mg/kg revealed a significant inhibitory effect (P < 0,01) in carrageenin-induced rat paw oedema and exhibited ulcer-protective properties against ethanol-induced ulceration in rats. An anti-diarrhoeal activity (P < 0.01) was also observed in castor-oil-induced diarrhoeal in mice. The intestinal transit was significantly (P < 0.01) reduced, however the pretreatment did not reduce the weight of intestinal contents. These results support the popular applications of Maytenus rigida for the treatment of inflammation, ulcer and diarrhoea in Brazil herbal traditional medicine.
O extrato etanólico bruto (EEOH) da casca de Maytenus rigida Mart (Celastraceae) uma planta da medicina popular do Brasil, foi testado para a atividade antiinflamatória, antiúlcera e antidiarréica em modelos animais. Não foi observado sinal de toxicidade aguda nos animais tratados com doses elevadas do EEOH (5000 mg/kg, v.o. ou 2000 mg/kg i.p.). O extrato nas doses de 250, 500 e 750 mg/kg mostrou um significante efeito inibitório (P < 0,01) no edema de pata induzido por carragenina e exibiu propriedade protetora contra a ulceração induzida por etanol em ratos. Também uma atividade antidiarréica (P < 0,01) foi observada na diarréia induzida por óleo de rícino em camundongos. O trânsito intestinal foi reduzido significativamente (P < 0.01), porém o pré-tratamento não reduziu o peso do conteúdo intestinal em ratos. Os resultados dão suporte à utilização de Maytenus rigida na medicina popular do Brasil para o tratamento da inflamação, da úlcera e da diarréia.