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通过制备介孔二氧化硅纳米颗粒固体分散体提高芹菜素的溶解度和生物利用度

Enhanced Solubility and Bioavailability of Apigenin via Preparation of Solid Dispersions of Mesoporous Silica Nanoparticles.

作者信息

Huang Yannian, Zhao Xiuhua, Zu Yuangang, Wang Lu, Deng Yiping, Wu Mingfang, Wang Huimei

机构信息

Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education Harbin, Heilongjiang 150040, China.

出版信息

Iran J Pharm Res. 2019 Winter;18(1):168-182.

PMID:31089353
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6487423/
Abstract

In this study, a novel mesoporous silica nanoparticles drug carrier contributes to improving the solubility, dissolution, and the oral bioavailability of apigenin (AP). The apigenin of solid dispersion of mesoporous silica nanoparticles (AP-MSN) was prepared by physical absorption method and also, drug release and bioavailability performance were evaluated. Based on its solubility, the AP-MSN solid dispersion was prepared at the weight ratio of 1:1 to obtain the optimum solubility. The loading efficiency (LE), encapsulation efficiency (EE), and solubility of AP-MSN solid dispersion were 29.71%, 42.27%, and 25.11 µg/mL, respectively. SEM, TEM, BET, FTIR, XRD, DSC, and TG were also carried out. These results demonstrated that AP was good absorbed into the pores of MSN through physical absorption effect of MSN. The DMF residues of AP-MSN solid dispersion meet the ICH requirements. It was vital that the AP-MSN solid dispersion behaved well and the accumulative release of AP-MSN solid dispersion was 2.37 times higher than that of raw AP. study, the AP area under curve was 8.32 times higher for the AP-MSN solid dispersion than that of raw AP, which indicated that the bioavailability of AP-MSN solid dispersion was greatly improved. Therefore, the prepared AP-MSN solid dispersion presents potential as a novel oral therapeutic agent formulation for clinical application.

摘要

在本研究中,一种新型的介孔二氧化硅纳米颗粒药物载体有助于提高芹菜素(AP)的溶解度、溶出度和口服生物利用度。通过物理吸附法制备了介孔二氧化硅纳米颗粒(AP-MSN)的芹菜素固体分散体,并对其药物释放和生物利用度性能进行了评估。基于其溶解度,以1:1的重量比制备AP-MSN固体分散体以获得最佳溶解度。AP-MSN固体分散体的载药效率(LE)、包封率(EE)和溶解度分别为29.71%、42.27%和25.11μg/mL。还进行了扫描电子显微镜(SEM)、透射电子显微镜(TEM)、比表面积分析(BET)、傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、差示扫描量热法(DSC)和热重分析(TG)。这些结果表明,通过MSN的物理吸附作用,AP很好地吸附到了MSN的孔中。AP-MSN固体分散体的二甲基甲酰胺残留量符合国际人用药品注册技术协调会(ICH)的要求。至关重要的是,AP-MSN固体分散体表现良好,其累积释放量比原料药AP高2.37倍。在研究中,AP-MSN固体分散体的药时曲线下面积比原料药AP高8.32倍,这表明AP-MSN固体分散体的生物利用度得到了极大提高。因此,所制备的AP-MSN固体分散体作为一种新型口服治疗剂制剂具有临床应用潜力。

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