Preparation and Characterization of Quercetin-Loaded Solid Dispersion by Solvent Evaporation and Freeze-Drying Method

IF 0.4 Q4 SPECTROSCOPY
S. H. Park, I. Song, Min‐Koo Choi
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引用次数: 5

Abstract

We prepared solid dispersion formulations of quercetin to enhance its solubility and dissolution rate. Various quercetinloaded solid dispersion were tested with quercetin, poloxamer 407, and carrier such as hydroxypropyl methyl cellulose (HPMC), polyethylene glycol 8000 (PEG 8000), and polyvinylpyrrolidone K40 (PVP K40) using solvent evaporation and freeze drying methods in terms of both the aqueous solubility and the dissolution rates of quercetin. The solubility of quercetin as its solid dispersion formulations was markedly improved compared with that of quercetin powder. Especially, highest solubility of quercetin was observed when HPMC was used as a carrier. The cumulative dissolution of quercetin within 360 min from solid dispersion composed of quercetin, poloxamer 407, and HPMC was 8.8-fold higher than the dissolution of pure quercetin. The results of powder Xray diffraction (XRD) and scanning electron microscope (SEM) indicated that quercetin transformed from a crystalline to an amorphous form through the solid dispersion formulation process. These results suggest that the solid dispersion formulation of quercetin with poloxamer 407 and HPMC could be a promising option for enhancing the solubility and dissolution rate of quercetin.
溶剂蒸发-冷冻干燥法制备槲皮素负载固体分散体及表征
为提高槲皮素的溶解度和溶出率,制备了槲皮素固体分散制剂。以槲皮素、poloxam407和羟丙基甲基纤维素(HPMC)、聚乙二醇8000 (PEG 8000)、聚乙烯吡咯烷酮K40 (PVP K40)为载体,采用溶剂蒸发和冷冻干燥的方法,对槲皮素的水溶性和溶出率进行了研究。槲皮素固体分散体的溶解度较槲皮素粉末有明显提高。特别是以HPMC为载体时,槲皮素的溶解度最高。槲皮素、poloxam407和HPMC组成的固体分散体在360 min内的累积溶出度是纯槲皮素的8.8倍。粉末x射线衍射(XRD)和扫描电镜(SEM)分析结果表明,槲皮素在固体分散配方过程中由结晶形态转变为无定形形态。上述结果表明,槲皮素与poloxam407和HPMC的固体分散是提高槲皮素溶解度和溶出率的一种有希望的选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
0.90
自引率
20.00%
发文量
0
审稿时长
6 weeks
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