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盐酸普萘洛尔-Eudragit RS100 电喷雾纳米制剂的形态和物理化学评价。

Morphological and physicochemical evaluation of the propranolol HCl-Eudragit RS100 electrosprayed nanoformulations.

机构信息

a Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.

b Drug Applied Research Center , Tabriz University of Medical Sciences , Tabriz , Iran.

出版信息

Artif Cells Nanomed Biotechnol. 2018 Jun;46(4):749-756. doi: 10.1080/21691401.2017.1337027. Epub 2017 Jun 6.

Abstract

The aim of this study was to fabricate propranolol hydrochloride (Prop. HCl) (as a water-soluble drug):Eudragit RS100 (Eud) nanobeads and nanofibres applying the electrospraying method as an economical and one-step technique. Different ratios of Prop. HCl:Eud (i.e. 1:5 and 1:10) at total solution concentrations of 10-20% W/V were investigated. The FE-SEM studies revealed that morphology and size of the samples were highly affected by the solution concentration; so that, the nanobeads (a mean diameter of 82.9 nm) were formed in low concentration and at the highest concentration of the solution, nanofibres (a mean diameter of 232.3 nm) were resulted. Besides the morphological changes, the size of processed nanoformulations was increased with an increment of the solution concentrations. X-ray diffraction results as well as DSC thermograms clearly indicated that the drug crystallinity decreased in the electrosprayed samples. Furthermore, in vitro dissolution test showed that the electrosprayed samples had relatively slower release patterns toward the pure drug and physical mixtures, where the samples with the drug:polymer ratio of 1:10 indicated a faster release rate toward 1:5 ratio; nevertheless, the concentration of the injected formulations did not remarkably impressed the release behaviours. The current study established the suitability of electrospraying method in the fabrication of the water-soluble drugs nanobeads/nanofibres; however, in vivo effectiveness of the prepared nanoformulations should be meticulously considered.

摘要

本研究旨在应用电喷射方法制备盐酸普萘洛尔(Prop. HCl)(水溶性药物):Eudragit RS100(Eud)纳米珠和纳米纤维,作为一种经济且一步法技术。研究了不同比例的 Prop. HCl:Eud(即 1:5 和 1:10)在总溶液浓度为 10-20%W/V 的情况下。FE-SEM 研究表明,样品的形态和尺寸受溶液浓度的影响很大;因此,在低浓度下形成纳米珠(平均直径为 82.9nm),在溶液浓度最高时形成纳米纤维(平均直径为 232.3nm)。除了形态变化外,处理后的纳米制剂的尺寸随着溶液浓度的增加而增加。X 射线衍射结果和 DSC 热图清楚地表明,药物结晶度在电喷射样品中降低。此外,体外溶解试验表明,电喷射样品对纯药物和物理混合物具有相对较慢的释放模式,其中药物:聚合物比为 1:10 的样品显示出比 1:5 比例更快的释放速率;然而,注入制剂的浓度对释放行为没有显著影响。本研究确立了电喷射方法在制备水溶性药物纳米珠/纳米纤维中的适用性;然而,应仔细考虑所制备的纳米制剂的体内效果。

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