RÉSUMÉ
Abstract Hesperidin is a natural compound which is found in citric fruits and presents antitumor and antimicrobial activities. However, the in vivo efficacy of Hesperidin is reduced due to its low oral bioavailability. Protein-based nanoparticles have been applied to improve biological parameters of drugs and natural compounds. Gliadin is a monomeric protein present in wheat. In this study, gliadin-based nanoparticles containing hesperidin were obtained by desolvation technique and a Taguchi orthogonal array design was employed to optimize the formulation. The independent variables were set as concentration of CaCl2 (0.5; 1 or 2%) and stabilizing agent (Pluronic F68, Tween 80 or sodium caseinate). The dependent variables consisted of mean diameter, polydispersity index, zeta potential, and encapsulation efficiency. The results showed significant effects on the dependent variables when 1% CaCl2 and Pluronic F68 were used. The optimized formulation was coated with chitosan to increase the physical stability of the nanoparticles. The final nanoparticles presented a mean diameter of 321 nm and polydispersity index of 0.217, and spherical shape. After coating, the Zeta potential was +21 mV, and the encapsulation efficiency was 73 %. The in vitro release assay showed that about 98% of the drug was released from the nanoparticles after 48 h. Moreover, the nanoparticles reduced hesperidin cytotoxicity on healthy cells (Vero cells) and improved the cytotoxicity on tumor cells (HeLa, PC-3 and Caco-2 cells). Results showed that the chitosan-coated gliadin nanoparticles are potential carriers for hesperidin delivery for cancer treatment.
Sujet(s)
Chitosane/composition chimique , Gliadine/composition chimique , Hespéridine/pharmacologie , Tumeurs/traitement médicamenteux , NanoparticulesRÉSUMÉ
SUMMARY OBJECTIVE: We studied the users of the Specialized Drug Distribution Program of the public health network. METHODS: A prospective cohort examined the elderly at two intervals of three years and included 30 patients in phase I and 16 in phase II. The methodology was composed of home visits, anthropometric, nutritional and hematological evaluation. For the progression of AD, the Clinical Dementia Rating (CDR) scale was used. RESULTS: According to the CDR, the disease evolved, since in 2014 most of the patients were in CDR 3. In the analysis of the micronutrients, only the B vitamins (B1, B2, B3, B5, B6) presented a significant reduction in 2014. The consumption of carbohydrates and lipids increased in the 2014 evaluation, and protein consumption decreased. As for the average weight of the elderly, there was an increase in 2014, 65.9 (± 15.6) Kg, with a BMI of 26.75 (± 4, 5), in 2011 the average weight was 62.44 kg (± 14, 36), BMI 24.64 (± 4.97). CONCLUSION: The hypothesis that patients are likely to be overweight or obese before the development of AD and that this may be associated with an increased risk of dementia is suggested.
RESUMO OBJETIVO: Foram estudados os usuários do programa de distribuição de medicamentos especializados da rede pública de saúde de Guarapuava, Paraná, Brasil. MÉTODOS: Uma coorte prospectiva, em que os idosos foram examinados em dois momentos, com um intervalo de três anos, com 30 pacientes na fase I e 16 na fase II. A metodologia foi composta por visitas domiciliares, avaliação antropométrica; avaliação nutricional e hematológica. Para a progressão da DA, utilizou-se a escala Clinical Demential Rating (CDR). Os testes de Shapiro-Wilk, teste de Wilcoxon e correlações com associações (Δ%), p < 0,05 para as análises estatísticas. RESULTADOS: A progressão da doença, segundo o CDR, evoluiu, pois, em 2014, a maioria dos pacientes encontrava-se em CDR 3. Na análise dos micronutrientes, somente as vitaminas do complexo B (B1, B2, B3, B5, B6) apresentaram redução significativa em 2014. O consumo de carboidratos e lipídeos aumentou na avaliação de 2014, e o consumo de proteínas diminuiu. Quanto ao peso médio dos idosos, houve um aumento em 2014, 65,9 (± 15,6) kg, com IMC 26,75 (± 4, 5); em 2011, o peso médio foi 62,44 kg (± 14,36), IMC 24,64 (± 4,97). CONCLUSÃO: Não foram encontrados pacientes anêmicos ou desnutridos na amostra. A hipótese de que os pacientes provavelmente já apresentavam sobrepeso ou obesidade antes do desenvolvimento da DA, e que isso pode estar associado com um aumento de risco de demência, pode ser sugerida.