Abstract

The self-nanoemulsifying drug delivery system has shown many advantages in drug delivery. In this study, a self-nanoemulsifying drug delivery system of buckwheat flavonoids was prepared for enhancing its antioxidant activity and oral bioavailability. A nanoemulsion of buckwheat flavonoids was developed and characterized, and its antioxidant, in vitro release, and in vivo bioavailability were determined. The nanoemulsion was optimized by the central composite design response surface experiment, and its particle size, polymer dispersity index (PDI), zeta potential, morphology, encapsulation efficiency, and stability were evaluated. The antioxidant activity was tested by measuring its 2,2-diphenyl-1-picrylhydrazyl scavenging activity, hydroxyl radical scavenging activity, and superoxide anion scavenging ability. In vitro release of buckwheat flavonoids nanoemulsion showed a higher cumulative release than the suspension, and the release fitting model followed the Ritger–Peppas and Weibull models. The effective concentration of the nanoemulsion was evaluated in vivo using a Wistar rat model, and the area under the plasma concentration-time curve of the buckwheat flavonoids nanoemulsion was 2.2-fold higher than that of the buckwheat flavonoid suspension. The C_max of the nanoemulsion was 2.6-fold greater than that of the suspension. These results indicate that the nanoemulsion is a promising oral drug delivery system that can improve the oral bioavailability to satisfy the clinical requirements.

中文翻译：

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荞麦类黄酮的自纳米乳化药物递送系统（SNEDDS）的制备，表征和抗氧化活性及生物利用度评估

摘要

自纳米乳化的药物递送系统在药物递送中显示出许多优点。在这项研究中，荞麦黄酮的自纳米乳化药物递送系统被制备以增强其抗氧化活性和口服生物利用度。荞麦黄酮的纳米乳液的开发和表征，其抗氧化剂，体外释放和体内测定生物利用度。通过中央复合设计响应表面实验对纳米乳液进行了优化，并对其粒径，聚合物分散指数（PDI），ζ电势，形态，包封效率和稳定性进行了评估。通过测量其2，2-二苯基-1-吡啶并肼基清除活性，羟基自由基清除活性和超氧阴离子清除能力来测试抗氧化剂活性。荞麦类黄酮纳米乳的体外释放显示出比悬浮液更高的累积释放，释放拟合模型遵循Ritger-Peppas和Weibull模型。在体内评估了纳米乳液的有效浓度使用Wistar大鼠模型，荞麦类黄酮纳米乳的血浆浓度-时间曲线下面积比荞麦类黄酮悬浮液高2.2倍。纳米乳液的C _max比悬浮液的C _max高2.6倍。这些结果表明，纳米乳剂是有希望的口服药物递送系统，其可以改善口服生物利用度以满足临床需求。