Poor bioavailability of hesperidin (HES) due to its gastric instability and low aqueous solubility limits its clinical application. The objective of presented work was to incorporate self-microemulsifying drug delivery system of HES (SMEDDS-HES) into alginate beads. The alginate beads were characterized for their size and morphology by using motic microscopy and scanning electron microscopy. The selected beads formulation (BF 7) revealed particle size (1.3 ± 0.117 mm), entrapment efficiency (87.4 ± 2.2%), circularity (0.9987), aspect ratio (0.9950), and swelling index (81.75 ± 2.14%). The encapsulation of HES in beads was assured by Fourier transform infrared spectroscopy study. The in vitro drug release kinetic of beads was performed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The results revealed negligible release of HES (3.52 ± 0.8%) from beads in SGF after 2 h, and in SIF (after 8 h), the beads showed burst release (72.52 ± 3.5%) of HES. Antidiabetic and histopathological studies on experimental rat revealed promising hypoglycemic activity of beads which sought for its ability to protect HES in the stomach. The shelf life of optimized bead formulation was estimated 1079 days suggesting excellent stability of HES after encapsulation. Finally, developed beads formulation was considered a promising approach in oral delivery of HES.

中文翻译：

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海藻酸钠微珠中橙皮苷自微乳化营养输送系统的制备以引起胃稳定性

由于橙皮苷（HES）的胃不稳定性和低水溶性，其生物利​​用度差限制了其临床应用。所提出工作的目的是将 HES (SMEDDS-HES) 的自微乳化给药系统纳入藻酸盐珠中。通过使用运动显微镜和扫描电子显微镜对藻酸盐珠粒的大小和形态进行表征。选定的珠子配方 (BF 7) 显示粒径 (1.3 ± 0.117 mm)、截留效率 (87.4 ± 2.2%)、圆形度 (0.9987)、纵横比 (0.9950) 和膨胀指数 (81.75 ± 2.14%)。傅里叶变换红外光谱研究确保了小珠中 HES 的封装。微丸的体外药物释放动力学在模拟胃液 (SGF) 和模拟肠液 (SIF) 中进行。结果显示，2 小时后，SGF 中的珠粒中 HES (3.52 ± 0.8%) 的释放可以忽略不计，而在 SIF 中（8 小时后），珠粒显示出 HES 的突释 (72.52 ± 3.5%)。对实验大鼠的抗糖尿病和组织病理学研究揭示了珠子有希望的降血糖活性，这些珠子寻求其保护胃中 HES 的能力。优化的珠子配方的保质期估计为 1079 天，表明封装后 HES 具有出色的稳定性。最后，开发的珠子配方被认为是口服 HES 的一种有前途的方法。对实验大鼠的抗糖尿病和组织病理学研究揭示了珠子有希望的降血糖活性，这些珠子寻求其保护胃中 HES 的能力。优化的珠子配方的保质期估计为 1079 天，表明封装后 HES 具有出色的稳定性。最后，开发的珠子配方被认为是口服 HES 的一种有前途的方法。对实验大鼠的抗糖尿病和组织病理学研究揭示了珠子有希望的降血糖活性，这些珠子寻求其保护胃中 HES 的能力。优化的珠子配方的保质期估计为 1079 天，表明封装后 HES 具有出色的稳定性。最后，开发的珠子配方被认为是口服 HES 的一种有前途的方法。