RESUMO
PURPOSE: Drugs used in the treatment of diseases can cause several unwanted systemic side effects. A site-specific drug delivery system can eliminate such consequences by delivering drugs to certain target areas of the body where therapeutic effects are required. Here we present the preparation and evaluation of magnetic nanoparticles of capsaicin, the active ingredient in chili peppers, coated with poly-L-lactide co-glycolide (PLGA), a FDA-approved biodegradable bioavailable polymer. METHODS: PCMN were prepared by solvent-evaporation/coprecipitation technique and their physicochemical and pharmacological characteristics evaluated in vitro. Further, effective pain/inflammation therapeutics of PCMN in a mouse model of inflammation was also studied. We also prepared and evaluated the subcellular localization of PLGA coated fluorescence magnetic nanoparticle (PFMN) in vitro in HEK293 cells. RESULTS: Transmission electron microscopic images of PCMN showed that the size of the nanoparticles were of the order of 10-20 nm. PCMN showed approximately 9.29% drug loading and 89.15% encapsulation efficiencies. In vitro dissolution studies showed an increased solubility of capsaicin due to the nano-size of the PCMN, while PLGA coating allowed sustained release of capsaicin in vitro. The PCMN also reduced paw edema after injection in mice, and confocal microscopy revealed the successful intracellular localization of PLGA-coated fluorescein magnetic nanoparticles in HEK293 cells. CONCLUSION: The PCMN provided a sustained release of capsaicin in vitro and inhibited carrageenan-induced inflammatory pain in mouse model in vivo. These data suggest that PLGA coating of capsaicin magnetic nanoparticles have the potential to be amenable for a sustained release of capsaicin to relieve pain.
Assuntos
Capsaicina/farmacologia , Ácido Láctico/química , Nanopartículas de Magnetita/química , Dor/tratamento farmacológico , Ácido Poliglicólico/química , Animais , Capsaicina/química , Sobrevivência Celular/efeitos dos fármacos , Preparações de Ação Retardada , Portadores de Fármacos , Liberação Controlada de Fármacos , Fluoresceína/química , Corantes Fluorescentes/química , Células HEK293 , Humanos , Inflamação/tratamento farmacológico , Masculino , Camundongos Endogâmicos C57BL , Tamanho da Partícula , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Solubilidade , Propriedades de SuperfícieRESUMO
We investigate experimentally and theoretically diffusiophoretic separation of negatively charged particles in a rectangular channel flow, driven by CO2 dissolution from one side-wall. Since the negatively charged particles create an exclusion zone near the boundary where CO2 is introduced, we model the problem by applying a shear flow approximation in a two-dimensional configuration. From the form of the equations we define a similarity variable to transform the reaction-diffusion equations for CO2 and ions and the advection-diffusion equation for the particle distribution to ordinary differential equations. The definition of the similarity variable suggests a characteristic length scale for the particle exclusion zone. We consider height-averaged flow behaviors in rectangular channels to rationalize and connect our experimental observations with the model, by calculating the wall shear rate as functions of channel dimensions. Our observations and the theoretical model provide the design parameters such as flow speed, channel dimensions and CO2 pressure for the in-flow water cleaning systems.