Apigenin (APG) is a very well-known flavonoid for its anti-inflammatory and anticancer properties. The purpose of this study is to improve the solubility and bioavailability of APG using a stable bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS). APG was incorporated in an oil phase comprising coconut oil fatty acid, Imwitor 988, Transcutol P, and HCO30 to form a Bio-SNEDDS. This preparation was characterized for morphology, particle size, and transmission electron microscopy (TEM). The APG performance was investigated in terms of loading, precipitation, release and stability tests from the optimal Bio-SNEDDS. An antimicrobial test was performed to investigate the activity of the Bio-SNEDDS against the selected strains. Bioavailability of the Bio-SNEDDS was evaluated using Wister rats against the commercial oral product and the pure drug. The results demonstrated the formation of an efficient nanosized (57 nm) Bio-SNEDDS with a drug loading of 12.50 mg/gm which is around 500-fold higher than free APG. TEM analysis revealed the formation of spherical and homogeneous nanodroplets of less than 60 nm. The dissolution rate was faster than the commercial product and was able to maintain 90% APG in gastro intestinal solution for more than 4 h. A stability study demonstrated that the Bio-SNEDDS is stable at a harsh condition. The in vivo pharmacokinetics parameters of the Bio-SNEDDS formulation in comparison to the pure drug showed a significant increase in maximum concentration (C_max) and area under the curve (AUC _(0–t)) of 105.05% and 91.32%, respectively. Moreover, the antimicrobial study revealed moderate inhibition in the bacterial growth rate. The APG-Bio-SNEDDS could serve as potential carrier aimed at improving the clinical application of APG.

中文翻译：

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使用生物活性自我纳米乳化药物递送系统（Bio-SNEDDS）增强芹菜素的口服生物利用度：体外，体内和稳定性评估。

芹菜素（APG）是一种非常著名的类黄酮，具有抗炎和抗癌的特性。这项研究的目的是使用稳定的生物活性自纳米乳化药物递送系统（Bio-SNEDDS）来提高APG的溶解度和生物利用度。将APG掺入包含椰子油脂肪酸，Imwitor 988，Transcutol P和HCO30的油相中以形成Bio-SNEDDS。对该制剂的形态，粒度和透射电子显微镜（TEM）进行了表征。根据最佳Bio-SNEDDS的负载，沉淀，释放和稳定性测试研究了APG的性能。进行了抗微生物测试，以研究Bio-SNEDDS对所选菌株的活性。使用Wister大鼠针对商业口服产品和纯药物评估Bio-SNEDDS的生物利用度。结果表明形成了有效的纳米级（57 nm）Bio-SNEDDS，其载药量为12.50 mg / gm，比游离APG高约500倍。TEM分析表明形成了小于60 nm的球形和均匀的纳米液滴。溶解速率比市售产品快，并且能够在胃肠溶液中维持90％APG超过4小时。稳定性研究表明，Bio-SNEDDS在恶劣条件下稳定。与纯药物相比，Bio-SNEDDS制剂的体内药代动力学参数显示最大浓度显着增加（C 结果表明形成了有效的纳米级（57 nm）Bio-SNEDDS，其载药量为12.50 mg / gm，比游离APG高约500倍。TEM分析表明形成了小于60 nm的球形和均匀的纳米液滴。溶解速度比市售产品快，并且能够在胃肠溶液中维持90％APG超过4小时。稳定性研究表明，Bio-SNEDDS在恶劣条件下稳定。与纯药物相比，Bio-SNEDDS制剂的体内药代动力学参数显示最大浓度显着增加（C 结果表明形成了有效的纳米级（57 nm）Bio-SNEDDS，其载药量为12.50 mg / gm，比游离APG高约500倍。TEM分析表明形成了小于60 nm的球形和均匀的纳米液滴。溶解速度比市售产品快，并且能够在胃肠溶液中维持90％APG超过4小时。稳定性研究表明，Bio-SNEDDS在恶劣条件下稳定。与纯药物相比，Bio-SNEDDS制剂的体内药代动力学参数显示最大浓度显着增加（C 溶解速度比市售产品快，并且能够在胃肠溶液中维持90％APG超过4小时。稳定性研究表明，Bio-SNEDDS在恶劣条件下稳定。与纯药物相比，Bio-SNEDDS制剂的体内药代动力学参数显示最大浓度显着增加（C 溶解速度比市售产品快，并且能够在胃肠溶液中维持90％APG超过4小时。稳定性研究表明，Bio-SNEDDS在恶劣条件下稳定。与纯药物相比，Bio-SNEDDS制剂的体内药代动力学参数显示最大浓度显着增加（C_max）和曲线下面积（AUC _（0–t））分别为105.05％和91.32％。此外，抗微生物研究显示细菌生长速率受到中等抑制。APG-Bio-SNEDDS可作为潜在载体，旨在改善APG的临床应用。