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, in-vitro drug release and in-vivo 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 in-vitro and the accumulative release of AP-MSN solid dispersion was 2.37 times higher than that of raw AP. In-vivo study, the AP area under curve0-t 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.

中文翻译：

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通过制备介孔二氧化硅纳米粒子的固体分散体，提高芹菜素的溶解度和生物利用度。

在这项研究中，新型的介孔二氧化硅纳米粒子药物载体有助于改善芹菜素（AP）的溶解度，溶解度和口服生物利用度。通过物理吸收法制备了介孔二氧化硅纳米颗粒（AP-MSN）固体分散体芹菜素，并对其体外释药和体内生物利用度进行了评价。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固体分散体的负载效率（LE），封装效率（EE）和溶解度分别为29.71％，42.27％和25.11 µg / mL。还进行了SEM，TEM，BET，FTIR，XRD，DSC和TG。这些结果表明，AP通过MSN的物理吸收作用被良好地吸收到MSN的孔中。AP-MSN固体分散体的DMF残留物符合ICH要求。至关重要的是，AP-MSN固体分散体在体外具有良好的性能，并且AP-MSN固体分散体的累积释放量是原始AP的2.37倍。体内研究表明，AP-MSN固体分散体的曲线0-t下的AP面积是原始AP的8.32倍，这表明AP-MSN固体分散体的生物利用度得到了很大的提高。因此，制备的AP-MSN固体分散体具有作为用于临床应用的新型口服治疗剂制剂的潜力。AP-MSN固体分散体的32倍于未加工的AP，这表明AP-MSN固体分散体的生物利用度得到了极大的提高。因此，制备的AP-MSN固体分散体具有作为用于临床应用的新型口服治疗剂制剂的潜力。AP-MSN固体分散体的32倍于未加工的AP，这表明AP-MSN固体分散体的生物利用度得到了极大的提高。因此，制备的AP-MSN固体分散体具有作为用于临床应用的新型口服治疗剂制剂的潜力。