PDF(Pubmed)
Abstract：
In various drug delivery systems, solid lipid nanoparticles are dominantly lipid-based nanocarriers. Amiodarone hydrochloride is an antiarrhythmic agent used to treat severe rhythm disturbances. It has variable and hard-to-predict absorption in the gastrointestinal tract because of its low solubility and high permeability. The aims of this study were to improve its solubility by encapsulating amiodarone into solid lipid nanoparticles using two excipients-Compritol® 888 ATO (pellets) (C888) as a lipid matrix and Transcutol® (T) as a surfactant. Six types of amiodarone-loaded solid lipid nanoparticles (AMD-SLNs) were obtained using a hot homogenization technique followed by ultrasonication with varying sonication parameters. AMD-SLNs were characterized by their size distribution, polydispersity index, zeta potential, entrapment efficiency, and drug loading. Based on the initial evaluation of the entrapment efficiency, only three solid lipid nanoparticle formulations (P1, P3, and P5) were further tested. They were evaluated through scanning electron microscopy, Fourier-transform infrared spectrometry, near-infrared spectrometry, thermogravimetry, differential scanning calorimetry, and in vitro dissolution tests. The P5 formulation showed optimum pharmaco-technical properties, and it had the greatest potential to be used in oral pharmaceutical products for the controlled delivery of amiodarone.
摘要：
在各种药物递送系统中，固体脂质纳米颗粒主要是基于脂质的纳米载体。盐酸胺碘酮是一种抗心律失常药，用于治疗严重的节律紊乱。由于其低溶解度和高渗透性，它在胃肠道中具有可变且难以预测的吸收。这项研究的目的是通过使用两种赋形剂-Compritol®888ATO（颗粒）（C888）作为脂质基质和Transcutol®（T）作为表面活性剂将胺碘酮包封到固体脂质纳米颗粒中来提高其溶解度。使用热均质化技术获得六种类型的负载胺碘酮的固体脂质纳米颗粒（AMD-SLN），然后使用不同的超声处理参数进行超声处理。AMD-SLN的特征在于它们的大小分布，多分散指数，zeta电位,截留效率，和药物装载。基于对截留效率的初步评估，仅三种固体脂质纳米颗粒制剂(P1、P3和P5)被进一步测试。通过扫描电子显微镜对它们进行了评估，傅里叶变换红外光谱法,近红外光谱法,热重分析,差示扫描量热法,和体外溶出度测试。P5配方显示出最佳的药物技术性能，并且它具有最大的潜力用于口服药物产品，用于控制胺碘酮的递送。
