RESUMO
Healthy weight loss represents a real challenge when obesity is increasing in prevalence. Herein, we report a conjugated polymer nanocarrier for smart deactivation of lipase and thus balancing calorie intake. After oral administration, the nanocarrier is sensitive to lipase in the digestive tract and releases orlistat, which deactivates the enzyme and inhibits fat digestion. It also creates negative feedback to control the release of itself. The nanocarrier smartly regulates activity of the lipase cyclically varied between high and low levels. In spite of high fat diet intervention, obese mice receiving a single dose of the nanocarrier lose weight over eight days, whereas a control group continues the tendency to gain weight. Daily intragastric administration of the nanocarrier leads to lower weight of livers or fat pads, smaller adipocyte size, and lower total cholesterol level than that of the control group. Near-infrared fluorescence of the nanocarrier reveals its biodistribution.
Assuntos
Fármacos Antiobesidade , Portadores de Fármacos , Lactonas , Lipase/antagonistas & inibidores , Nanopartículas/química , Redução de Peso/efeitos dos fármacos , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacologia , Lactonas/química , Lactonas/farmacologia , Lipase/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , OrlistateRESUMO
Dextran modified with pendant acetals is used to load doxorubicin (DOX) and a near-infrared-emissive conjugated polymer (BTTPF), and this aims to provide selective drug release at therapeutic targets including tumors. The BTTPF is applicable to tracking the anticancer drug release through the change of Förster resonance energy transfer efficiency between doxorubicin and BTTPF during degradation of the nanoparticles in vivo.