DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Lecithin-based nanocapsule loading sucupira (Pterodon emarginatus) oil effects in experimental mucositis.(2022) Di Miceli, Jeruza Ferraz Filgueiras; Andrade, Maria Emília Rabelo; Carvalho, Paula Lopes Armond; Santos, Elandia Aparecida; Oliveira, Anna Eliza Maciel de Faria Mota; Fernandes, Caio Pinho; Cruz, Rodrigo Alves Soares; Garrett, Rafael; Mosqueira, Vanessa Carla Furtado; Cassali, Geovanni Dantas; D’Haese, Cecile; Nysten, Bernard; Leite, Jacqueline Isaura Alvarez; Cardoso, Valbert Nascimento; Araújo, Raquel SilvaIntestinal mucositis (IM) is a frequent adverse effect in anticancer therapy without standard treatment. The oil obtained from sucupira (Pterodon emarginatus) has anti-inflammatory properties, and the soybean lecithin re- duces the intestinal toxicity of several xenobiotics. However, their water insolubility impairs the in vivo appli- cation. For this reason, we evaluated if the nanoencapsulation of sucupira oil (SO) in lecithin-based nanocapsules (SO-NC) could be a therapeutically effective system for the treatment of IM in murine cisplatin (CDDP)-induced intestinal mucositis model. SO was analyzed by LC-HRMS/MS and HPLC. SO-NC was prepared by nano- precipitation and characterized using DLS, HPLC, and AFM. Mice body weight and food consumption were assessed daily during experimental mucositis induced by CDDP. The animals were euthanized, and intestinal permeability, inflammatory mediators, and intestinal histology were performed. SO-NC demonstrated adequate characteristics for oral administration as size under 300 nm, IP < 0.3, high EE, and spherical shape. In vitro cytotoxicity performed against RAW 264.7 cell lines resulted in cell viability above 80 % confirming the non- cytotoxic profile of SO (IC50 268 μg/mL) and SO-NC (IC50 118.5 μg/mL) up to 117.2 μg/mL. The untreated mice showed intestinal toxicity after i.p. of CDDP, principally weight loss, increased intestinal permeability, and MPO and TNF-α levels. Surprisingly, the administration of SO to CDDP-mucositis animals did not circumvent the CDDP effects and increased intestinal permeability. However, SO-NC proved efficient in mitigating the experi- mental intestinal mucositis by improving intestinal epithelium architecture, reducing intestinal permeability, and improving the MPO levels. In conclusion, SO-NC can positively impact intestinal mucositis by promoting mucosal recovery. This is a promising strategy for developing a new treatment for intestinal mucositis.Item Chemical characterization and anti-inflammatory assessment of the hydroethanolic extract of Fridericia chica.(2020) Takenaka, Isabella Kuniko Tavares Magalhães; Amorim, Juliana Mendes; Barros, Patrícia Aparecida Vieira de; Brandão, Geraldo Célio; Contarini, Sara Moreira Lopes; Melo, Éricka Lorenna de Sales Souza e; Leite, Camila Megale Almeida; Martins, Flaviano dos Santos; Cardoso, Valbert Nascimento; Castilho, Rachel Oliveira; Diniz, Simone Odília Antunes FernandesFridericia chica (Bonpl.) L.G. Lohmann, Bignoniaceae, is an Amazonian species known as “pariri” or “crajiru” that is included in the Brazilian National List of Medicinal Plants of Interest to the Unified Health System (Renisus). This herbal remedy is traditionally used as an infusion to treat diarrhea, anemia, inflammation, symptoms of mucositis, and frequent complications of chemotherapy. This study aimed to characterize the chemical profile of the hydroethanolic extract of F. chica and to assess its intestinal anti-inflammatory activity. The chemical profile of the leaves was determined by ultra-performance liquid chromatog raphy coupled to mass spectrometry, and its potential anti-inflammatory activity in the gut was evaluated in mucositis induced by 5-fluorouracil. Three novel compounds from this the species were identified 6,7,3′,4′-tetrahydroxy-5-methoxyflavilium-O-glu curonide, scutellarein-O-glucuronide, and 5-methyl-scutellarein-O-glucuronide, as well as flavones and anthocyanidins that have been previously described. Mice received the hydroethanolic extract (300 mg/kg) for 9 days, and no signs of toxicity were observed. After 72 h of 5-fluorouracil administration, intestinal permeability, bacterial translocation, myeloperoxidase activity, eosinophil peroxidase activity, and histological analyses were performed. Treatment with the analyzed extract was beneficial, as it normalized intestinal permeability, bacterial translocation, myeloperoxidase activity/eosinophil peroxidase and preserved intestinal epithelium architecture. This study provides new insights into the chemical composition and biological activity of the polar extracts from “pariri”, an important Amazonian crude medicinal drug.Item Effect of pH, mucin and bovine serum on rifampicin permeability through Caco-2 cells.(2012) Gonçalves, José Eduardo; Fernandes, Mariane Ballerini; Chiann, Chang; Gai, Maria Nella; Souza, Jacqueline de; Storpirtis, SílviaRifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intestinal mucosa to assess the uptake and transport of rifampicin and the effects of various experimental conditions were investigated, in order to establish the influence of these variables on rifampicin permeability. Different pHs (5.8, 6.8 and 7.4) in the apical medium, the presence or absence of mucin (3.0% w/v) in the donor site and the presence or absence of bovine serum albumin (4.0% v/v) in the receptor chamber were the evaluated conditions. The quantification of rifampicin in the apical or basolateral chambers was performed by a validated HPLC-UV method. The change in the donor chamber pH showed that permeability values were greater at pH 6.8, although this increase does not result in an alteration of the qualitative classification of rifampicin, which has high permeability. Mucin and bovine serum showed no effects on the permeability of rifampicin at the concentration tested. Overall, the current study suggests that pH, artificial mucin and bovine serum proteins have no influence on rifampicin permeability.