PDF(Pubmed)
Abstract：
UNASSIGNED: Oxyberberine (OBB), one of the main metabolites of berberine derived from intestinal and erythrocyte metabolism, exhibits appreciable anti-hyperuricemic activity. However, the low water solubility and poor plasma concentration-effect relationship of OBB hamper its development and utilization. Therefore, an OBB-hydroxypropyl-β-cyclodextrin (HP-β-CD) supersaturated drug delivery system (SDDS) was prepared and characterized in this work.
UNASSIGNED: OBB-HP-β-CD SDDS was prepared using the ultrasonic-solvent evaporation method and characterized. Additionally, the in vitro and in vivo release experiments were conducted to assess the release kinetics of OBB-HP-β-CD SDDS. Subsequently, the therapeutic efficacy of OBB-HP-β-CD SDDS on hyperuricemia (HUA) was investigated by means of histopathological examination and evaluation of relevant biomarkers.
UNASSIGNED: The results of FT-IR, DSC, PXRD, NMR and molecular modeling showed that the crystallized form of OBB was transformed into an amorphous OBB-HP-β-CD complex. Dynamic light scattering indicated that this system was relatively stable and maintained by formation of nanoaggregates with an average diameter of 23 nm. The dissolution rate of OBB-HP-β-CD SDDS was about 5 times higher than that of OBB raw material. Furthermore, the AUC0-t of OBB-HP-β-CD SDDS (10.882 μg/mL*h) was significantly higher than that of the raw OBB counterpart (0.701 μg/mL*h). The oral relative bioavailability of OBB-HP-β-CD SDDS was also enhanced by 16 times compared to that of the raw material. Finally, in vivo pharmacodynamic assay showed the anti-hyperuricemic potency of OBB-HP-β-CD SDDS was approximately 5-10 times higher than that of OBB raw material.
UNASSIGNED: Based on our findings above, OBB-HP-β-CD SDDS proved to be an excellent drug delivery system for increasing the solubility, dissolution, bioavailability, and anti-hyperuricemic potency of OBB.
UNASSIGNED: OBB-HP-β-CD SDDS was prepared using the ultrasonic-solvent evaporation method and characterized. Additionally, the in vitro and in vivo release experiments were conducted to assess the release kinetics of OBB-HP-β-CD SDDS. Subsequently, the therapeutic efficacy of OBB-HP-β-CD SDDS on hyperuricemia (HUA) was investigated by means of histopathological examination and evaluation of relevant biomarkers.
UNASSIGNED: The results of FT-IR, DSC, PXRD, NMR and molecular modeling showed that the crystallized form of OBB was transformed into an amorphous OBB-HP-β-CD complex. Dynamic light scattering indicated that this system was relatively stable and maintained by formation of nanoaggregates with an average diameter of 23 nm. The dissolution rate of OBB-HP-β-CD SDDS was about 5 times higher than that of OBB raw material. Furthermore, the AUC0-t of OBB-HP-β-CD SDDS (10.882 μg/mL*h) was significantly higher than that of the raw OBB counterpart (0.701 μg/mL*h). The oral relative bioavailability of OBB-HP-β-CD SDDS was also enhanced by 16 times compared to that of the raw material. Finally, in vivo pharmacodynamic assay showed the anti-hyperuricemic potency of OBB-HP-β-CD SDDS was approximately 5-10 times higher than that of OBB raw material.
UNASSIGNED: Based on our findings above, OBB-HP-β-CD SDDS proved to be an excellent drug delivery system for increasing the solubility, dissolution, bioavailability, and anti-hyperuricemic potency of OBB.
摘要：
■氧连素（OBB），小檗碱的主要代谢产物之一来自肠道和红细胞代谢，表现出明显的抗高尿酸活性。然而,OBB的水溶性低和血浆浓度-效应关系差阻碍了其开发和利用。因此,制备了OBB-羟丙基-β-环糊精（HP-β-CD）过饱和药物传递系统（SDDS），并对其进行了表征。
■使用超声-溶剂蒸发法制备了OBB-HP-β-CDSDDS，并对其进行了表征。此外,进行了体外和体内释放实验以评估OBB-HP-β-CDSDDS的释放动力学。随后，通过组织病理学检查和相关生物标志物评估,研究了OBB-HP-β-CDSDDS对高尿酸血症(HUA)的疗效.
■FT-IR的结果，DSC,PXRD,NMR和分子模拟显示OBB的结晶形式转化为无定形OBB-HP-β-CD复合物。动态光散射表明该体系相对稳定，并通过形成平均直径为23nm的纳米聚集体而得以维持。OBB-HP-β-CDSDDS的溶出速率比OBB原料高约5倍。此外，OBB-HP-β-CDSDDS的AUC0-t（10.882μg/mL*h）显着高于原始OBB对应物（0.701μg/mL*h）。OBB-HP-β-CDSDDS的口服相对生物利用度也比原料药提高了16倍。最后,体内药效学试验表明，OBB-HP-β-CDSDDS的抗高尿酸血症效力比OBB原料高约5-10倍。
■根据我们上面的发现，OBB-HP-β-CDSDDS被证明是一种优异的药物递送系统，用于增加溶解度，溶出度,生物利用度，和OBB的抗高尿酸血症效力。
■使用超声-溶剂蒸发法制备了OBB-HP-β-CDSDDS，并对其进行了表征。此外,进行了体外和体内释放实验以评估OBB-HP-β-CDSDDS的释放动力学。随后，通过组织病理学检查和相关生物标志物评估,研究了OBB-HP-β-CDSDDS对高尿酸血症(HUA)的疗效.
■FT-IR的结果，DSC,PXRD,NMR和分子模拟显示OBB的结晶形式转化为无定形OBB-HP-β-CD复合物。动态光散射表明该体系相对稳定，并通过形成平均直径为23nm的纳米聚集体而得以维持。OBB-HP-β-CDSDDS的溶出速率比OBB原料高约5倍。此外，OBB-HP-β-CDSDDS的AUC0-t（10.882μg/mL*h）显着高于原始OBB对应物（0.701μg/mL*h）。OBB-HP-β-CDSDDS的口服相对生物利用度也比原料药提高了16倍。最后,体内药效学试验表明，OBB-HP-β-CDSDDS的抗高尿酸血症效力比OBB原料高约5-10倍。
■根据我们上面的发现，OBB-HP-β-CDSDDS被证明是一种优异的药物递送系统，用于增加溶解度，溶出度,生物利用度，和OBB的抗高尿酸血症效力。
