RESUMO
The main objective of this study was to evaluate the potential of quercetin-loaded nanostructured lipid carriers (QT-NLCs) as a topical delivery system. QT-NLCs were prepared by the method of emulsion evaporation-solidification at low temperature. The average entrapment efficiency and drug loading of the optimized QT-NLCs were 89.95 ± 0.16% and 3.05 ± 0.01%, respectively. Under the transmission electron microscope, the nanoparticles were spherically shaped. The average particle size was 215.2 nm, the zeta potential was -20.10 ± 1.22 mV and pH value of QT-NLCs system was 4.65. Topical delivery of QT in the form of NLCs was investigated in vitro and in vivo. The results showed that QT-NLCs could promote the permeation of QT, increase the amount of QT retention in epidermis and dermis, and enhance the effect of anti-oxidation and anti-inflammation exerted by QT. Then the mechanism of NLCs for facilitating drug penetration was further investigated through histological sections. In conclusion, NLCs could be a promising vehicle for topical delivery of QT.
Assuntos
Anti-Inflamatórios/administração & dosagem , Portadores de Fármacos , Edema/prevenção & controle , Sequestradores de Radicais Livres/administração & dosagem , Lipídeos/química , Nanoestruturas , Quercetina/administração & dosagem , Administração Tópica , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/metabolismo , Química Farmacêutica , Preparações de Ação Retardada , Modelos Animais de Doenças , Composição de Medicamentos , Edema/induzido quimicamente , Edema/metabolismo , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/metabolismo , Masculino , Camundongos , Microscopia Eletrônica de Transmissão , Nanotecnologia , Tamanho da Partícula , Permeabilidade , Quercetina/química , Quercetina/metabolismo , Pele/efeitos dos fármacos , Pele/metabolismo , Pele/patologia , Absorção Cutânea , Solubilidade , Superóxidos/química , Tecnologia Farmacêutica , Temperatura , XilenosRESUMO
The purpose of this study was to investigate the preparation and characteristics of curcumin phospholipid complex, including the effects of reaction time, reaction solvent, reaction concentration and reaction temperature. Preparation technology resulted in that 0.5 g curcumin and 10 g soy phospholipid dissolved in 100 mL anhydrous alcohol, were stirred 1 h in 50 degrees C waterbath, then steamed alcohol in decompression, collected solid residue and vacuum dried for 12 h. The physicochemical properties for the new complex including IR spectrometer, mass spectrograph and HNMR equipment were detected. As a result, the formation of the complex is based on the reaction between phospholipid polar group rounding phosphorus atom and curcumin. This result gave the evidence for the formation mechanism of phospholipid complex.
