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1.
Eur J Pharm Biopharm ; 163: 16-22, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33774161

RESUMO

In vivo evaluation of arabinoxylans (AX) microspheres showed to protect insulin from degradation in the upper gastrointestinal tract and carrier insulin to colon. Insulin-loaded AX microspheres (50 UI/kg) decreased blood glucose level by 39% in diabetic rats with a maximum effect at 18 h post-administration, indicating that insulin remains bioactive. The continuous administration (4 days) of insulin-loaded AX microspheres improved the polyuria and increased the production of short-chain fatty acids, as well as Bifidobacterium and Bacteroides in diabetic rats compared to untreated diabetic rats. AX microspheres are a potential microbiota-activated carrier for colon-specific drug delivery and could be useful as a complementary treatment for diabetes.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Portadores de Fármacos/metabolismo , Microbioma Gastrointestinal , Insulina/administração & dosagem , Xilanos/metabolismo , Administração Oral , Animais , Colo/metabolismo , Colo/microbiologia , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/microbiologia , Diabetes Mellitus Tipo 1/induzido quimicamente , Diabetes Mellitus Tipo 1/microbiologia , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/microbiologia , Humanos , Insulina/farmacocinética , Mucosa Intestinal/metabolismo , Mucosa Intestinal/microbiologia , Masculino , Microesferas , Ratos , Estreptozocina/administração & dosagem , Estreptozocina/toxicidade
2.
Int J Biol Macromol ; 126: 952-959, 2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30584929

RESUMO

Arabinoxylans (AX) microspheres with different insulin/AX mass ratio were prepared by formation of phenoxy radical issued from the ferulic acid by enzymatic oxidation (entrapped in situ of insulin). Phenolic acid content and FT-IR spectrum of unloaded and insulin-loaded AX microspheres revealed that the phenoxy radical issued from the ferulic acid by enzymatic oxidation did not interact covalently with insulin. The microspheres showed a spherical shape, smooth surface and an average diameter of particles of 320 µm. In vitro control release found that AX microspheres minimized the insulin loss in the upper GI tract, retaining high percentage (~75%) of insulin in its matrix. The stability of the secondary structure of insulin was studied by dichroism circular (CD). The CD spectra of insulin released from AX microspheres did not change according to the insulin/AX mass ratio of the microsphere. Significant hypoglycemic effects with improved insulin-relative bioavailability tested on an in vivo murine model revealed the efficacy of these enzymatically cross-linked arabinoxylans microspheres as a new oral insulin carrier.


Assuntos
Reagentes de Ligações Cruzadas/química , Sistemas de Liberação de Medicamentos , Insulina/administração & dosagem , Lacase/metabolismo , Microesferas , Xilanos/química , Administração Oral , Animais , Glicemia/metabolismo , Liberação Controlada de Fármacos , Humanos , Masculino , Ratos Wistar , Reologia , Espectroscopia de Infravermelho com Transformada de Fourier , Distribuição Tecidual
3.
J Agric Food Chem ; 49(2): 946-51, 2001 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-11262054

RESUMO

Flame Seedless grapes were sprayed with N-(2-chloro-4-pyridyl)-N-phenylurea (CPPU) at 0, 2.5, and 5.0 ppm to develop rachis resistant to browning and dehydration. Rachis polyphenol oxidase (PPO) activity was determined during cluster development. Cluster components were weighed at commercial (CM), and physiological maturity (PM). PPO activity, rachis color changes (L and a), and cluster weight loss were evaluated at 0 degrees C for 8, 16, 32, and 56 days. CPPU-treated rachis had a decrease of 36% in PPO activity and a week delay in peak activity. At PM, dry weight of CPPU-treated rachis increased by 3 g. Postharvest rachis PPO activity declined with CPPU application, and color changes followed the same pattern for CM and PM. After 32 days of storage, L and a in lateral branches were significantly superior in CPPU treatments. Weight losses below 2.1% were significantly lowest in CPPU-treated clusters for 16 days of storage regardless of cluster maturity.


Assuntos
Catecol Oxidase/metabolismo , Compostos de Fenilureia/farmacologia , Caules de Planta/enzimologia , Piridinas/farmacologia , Rosales/enzimologia , Catecol Oxidase/efeitos dos fármacos , Cor , Citocininas/farmacologia , Dessecação , Manipulação de Alimentos , Reação de Maillard/efeitos dos fármacos , Fatores de Tempo
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