莫达非尼的电喷涂聚合物纳米球和纳米纤维:制备、表征和药物释放研究

K. Adibkia, Sevil Selselehjonban, S. Emami, K. Osouli-Bostanabad, M. Barzegar-Jalali
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引用次数: 6

摘要

莫达非尼(MDF)用于口服治疗注意力缺陷/多动障碍和嗜睡症。它具有低溶解度和高渗透率;因此,通过制备纳米制剂来改善其溶出性能是提高其口服吸收的一种很有前途的方法。我们的目的是通过电喷雾技术制备和表征MDF-Eudragit®RS100 (MDF-ERS)纳米颗粒。方法:通过改变MDF与ERS的比例和浓度制备电喷涂纳米颗粒。采用扫描电镜(SEM)、差示扫描量热法(DSC)、粉末x射线衍射(PXRD)和傅里叶变换红外光谱(FTIR)对配方进行了表征。对纳米颗粒、物理混合物和原料MDF进行了释放研究。将释放数据拟合到不同的模型中,以了解药物释放的机制。结果:电喷涂MDF和ERS溶液可以制备出非纤维或纳米纤维,所得产物的颗粒特性在很大程度上受溶液中聚合物用量的控制。PXRD和热分析表明,MDF是纳米颗粒结构中的非晶相。利用FTIR,在纳米颗粒中未观察到MDF和ERS之间的相互作用。纳米颗粒呈双相释放,溶出速率顺序为:纳米纤维>MDF>纳米颗粒。拟合良好的模型为Weibull模型,表明释放机制以菲克式扩散为主。结论:通过对溶液浓度等参数的优化,可以制备出具有较高溶出率的MDF-ERS纳米纤维和纳米球。电喷雾沉积作为一种简单、连续、无表面活性剂的方法,是制备载药聚合物纳米颗粒的理想选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Electrosprayed polymeric nanobeads and nanofibers of modafinil: preparation, characterization, and drug release studies
Introduction: Modafinil (MDF) is used orally for the treatment of attention-deficit/hyperactivity disorder and narcolepsy. It holds low solubility and high permeability; therefore, improving its dissolution properties by preparing nanoformulations can be a promising approach to enhance its oral absorption. Our aims were to prepare and characterize MDF-Eudragit® RS100 (MDF-ERS) nanoparticles by electrospray technique. Methods: Electrosprayed nanoparticles were fabricated by varying MDF to ERS ratios and concentrations. The formulations were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FTIR). Release studies were performed on nanoparticles, physical mixtures, and raw MDF. The release data were fitted to different models to understand the mechanism of the drug release. Results: Electrospraying of MDF and ERS solution resulted in the preparation of nonobeads or nanofibers, and the particulate characteristics of the obtained products were largely controlled by the polymer amount in the solution. PXRD and thermal analyses showed that MDF was an amorphous phase in the structures of nanoparticles. Using FTIR, no interaction was observed between MDF and ERS in nanoparticles. Nanoparticles showed biphasic release profiles and the order of dissolution rates was: nanofibers>MDF>nanobeads. The well-fitted model was Weibull model, indicating a Fickian diffusion as the main mechanism of release. Conclusion: The results suggest that by optimization of variables such as solution concentration of MDF-ERS nanofibers and nanobeads with higher dissolution rates can be made by electrospray. Electrospray deposition as a simple, continuous, and surfactant free method is an excellent choice for preparation of drug loaded polymeric nanoparticles.
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