Development of iron/ethylcellulose (core/shell) nanoparticles loaded with diclofenac sodium for arthritis treatment

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• 作者：José ; L. Arias ; Margarita Ló ; pez-Viota ; Juliá ; n Ló ; pez-Viota ; Á ; ngel V. Delgado
• 关键词：Controlled drug delivery ; Diclofenac sodium ; Ethylcellulose ; Iron ; Magnetic colloids ; Stimuli-sensitive drug carriers
• 刊名：International Journal of Pharmaceutics
• 出版年：2009
• 出版时间：1 December 2009
• 年：2009
• 卷：382
• 期：1-2
• 页码：270-276
• 全文大小：694 K

文摘

Diclofenac sodium is a non-steroidal anti-inflammatory drug of choice to treat arthritis because of its potential anti-inflammatory and analgesic activity. Because of its shorter biological half-life, it is needed to be given frequently and at high doses to elicit the required therapeutic activity, simultaneously leading to severe side effects. We hypothesized that the efficient delivery of diclofenac sodium to inflammation using a magnetic colloid could reduce the dose required to bring out sufficient therapeutic response. Hence, we have developed a diclofenac sodium-loaded magnetic nanomedicine, consisting of a magnetic core (iron) and a biocompatible polymeric shell (ethylcellulose) for parenteral administration. These core/shell nanoparticles were synthesized by an emulsion solvent evaporation process. Two drug loading methods were analyzed: the first one being drug addition prior to the emulsion solvent evaporation process (leading to drug entrapment into the polymeric network), and the second method based on diclofenac sodium surface adsorption onto the preformed nanoparticles. Compared to drug adsorption, the entrapment of this active agent into the polymeric matrix yielded a higher drug loading and a slower drug release profile. Such nanocomposites possessed very important characteristics such as unusually high drug loading, enhanced magnetic susceptibility and prolonged drug release, indicating their potential use as nanocarriers for efficient delivery of diclofenac sodium to inflammation sites.