d-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)制备泊沙康唑纳米胶束及表征

Q3 Pharmacology, Toxicology and Pharmaceutics
Alaa abdul elah Abdulqader, Nawal A. Rajab Sultan
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引用次数: 0

摘要

泊沙康唑(Posaconazole, POCZ)是一种新开发的扩展谱三唑,属于BCS II类,溶解度小于1µg/ml。在免疫系统较弱的患者中,POCZ已被证明是一种有效的抗真菌治疗由念珠菌和曲霉引起的侵袭性感染。纳米胶束技术可以提高POCZ的溶解度。为了增加其在水中的表观溶解度,纳米胶束是由大分子组合而成的,这些大分子自组装成有序的结构,能够在内部区域内包裹疏水药物分子。分散胶体系统是一个庞大而多样的群体,纳米胶束是其中的一个子集。由本身分散在介质中的相组成的(连续相)。当表面活性剂在溶液中的浓度高于临界胶束浓度(CMC)时,表面活性剂会形成胶体溶液。用TPGS和t80制备了POCZ纳米胶束。在本研究中,我们制备了6种不同的配方,并分析了它们的粒径、多分散指数(PDI)、包封效率(EE)、载药量(DL)、饱和溶解度和体外释放度。对泊沙康唑配方(POCZ6)的载药纳米胶束进行了表征,结果表明:在TPGS: tween80(1:5:3)比下,其粒径(90.68 nm)、PDI(0.27)、EE(94%)、DL(10.3%)和最佳溶解度(1133)均优于纯药物;体外释放研究结果表明,所选择的配方POCZ6在70分钟内释放全剂量药物,而纯药的释放率仅为23%。傅里叶变换红外显微镜和其他形式的调查(FTIR)。从数据可以看出,泊沙康唑与聚合物和表面活性剂结合时,其主峰没有相互作用,也没有变化。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and characterization of Posaconazole as a Nano-micelles using d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS)
It is important to note that Posaconazole (POCZ) is a newly developed extended-spectrum triazole that belongs to BCS class II and has a solubility of less than 1µg/ml. In patients with a weakened immune system, POCZ has been shown to be effective as an antifungal treatment for invasive infections caused by candida and aspergillus species. The nano-micelles technique can be used to increase POCZ solubility. In order to increase their apparent solubility in water, nano-micelles are made by combining macromolecules that self-assemble into ordered structures capable of entrapping hydrophobic drug molecules in the interior domain. Dispersed colloidal systems, of which nano-micelles are a subset, are a large and diverse group. Composed of a phase that is itself dispersed throughout a medium (continuous phase). Surfactants form a colloidal solution when their concentration in solution is higher than their critical micelle concentration (CMC). POCZ nano-micelles are made with TPGS and tween 80. In this study, we prepared six different formulations and analyzed their particle size, polydispersity index (PDI), entrapment efficiency (EE), drug loadings (DL), saturation solubility, and in-vitro release. The drug-loaded nano-micelles of the Posaconazole formula (POCZ6) were characterized, and their properties were found to be: Particle size (90.68 nm), PDI (0.27), EE (94%), DL (10.3%), and best solubility factor (1133) are all better in the TPGS: tween80(1:5:3) ratio than in the pure drug. An in-vitro release study was conducted, and the results showed that the chosen formula POCZ6 released the entire dose of drug in 70 minutes, compared to only 23% for pure drug. Fourier transform infrared microscopy and other forms of investigation (FTIR). As can be seen from the data, there are no interactions or changes in the major peaks of Posaconazole when it is combined with polymer and surfactant.
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来源期刊
Iraqi Journal of Pharmaceutical Sciences
Iraqi Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.40
自引率
0.00%
发文量
37
审稿时长
24 weeks
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