用于胺碘酮控制递送的固体脂质纳米粒子的开发。

IF 2.3 Q3 BIOCHEMICAL RESEARCH METHODS
Andreea Creteanu, Gabriela Lisa, Cornelia Vasile, Maria-Cristina Popescu, Adrian Florin Spac, Gladiola Tantaru
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引用次数: 0

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。盐酸胺碘酮是一种用于治疗严重心律失常的抗心律失常药物。由于其低溶解度和高渗透性,它在胃肠道中的吸收是可变的,并且很难预测。本研究的目的是通过使用两种赋形剂Compritol®888 ATO(颗粒)(C888)作为脂质基质和Transcutol®(T)作为表面活性剂将胺碘酮封装到固体脂质纳米颗粒中来提高其溶解度。使用热均化技术,然后用不同的超声参数进行超声处理,获得了六种类型的胺碘酮负载的固体脂质纳米颗粒(AMD SLNs)。AMD SLNs通过其尺寸分布、多分散指数、ζ电位、包封效率和载药量进行表征。基于包封效率的初步评估,仅对三种固体脂质纳米颗粒制剂(P1、P3和P5)进行了进一步测试。通过扫描电子显微镜、傅立叶变换红外光谱、近红外光谱、热重分析、差示扫描量热法和体外溶出试验对它们进行了评价。P5制剂显示出最佳的药物技术性能,并且在胺碘酮的控制递送的口服药物产品中具有最大的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Development of Solid Lipid Nanoparticles for Controlled Amiodarone Delivery.

Development of Solid Lipid Nanoparticles for Controlled Amiodarone Delivery.

Development of Solid Lipid Nanoparticles for Controlled Amiodarone Delivery.

Development of Solid Lipid Nanoparticles for Controlled Amiodarone Delivery.

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.

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来源期刊
Methods and Protocols
Methods and Protocols Biochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (miscellaneous)
CiteScore
3.60
自引率
0.00%
发文量
85
审稿时长
8 weeks
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