Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayuthaya Road, Rajathevi, Bangkok, 10400, Thailand.
Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, 10400, Thailand.
Sci Rep. 2024 Apr 17;14(1):8851. doi: 10.1038/s41598-024-59617-z.
Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions. The droplet of diluted SNEDDS demonstrated a spherical shape with a size of less than 100 nm and a neutral charge. The very fast self-emulsification was obtained within 32 s, and the transmittance values exceeded 99%. The highest drug loading was 90.10 ± 0.24% of the initial load with the highest %encapsulation efficiency of 84.20 ± 0.03%. FT-IR and DSC spectra showed no interaction between components. The dissolution in buffer pH 1.2, 4.5, and 6.8 showed significantly higher dissolved apigenin than the apigenin coarse powder. The dissolution profiles were fitted to the Korsmeyer-Peppas kinetics. The cellular antioxidant activities in Caco-2 cells were approximately 52.25-54.64% compared to no treatment and were higher than the apigenin coarse powder (12.70%). Our work highlights the potential of SNEDDS to enhance the dissolution and permeability of apigenin and promote antioxidant efficacy, which has a strong chance of being developed as a bioactive compound for nutraceuticals.
自微乳药物传递系统(SNEDDS)已被用于改善各种药物的口服生物利用度。在本研究中,开发了芹菜素 SNEDDS 来解决其溶解问题并提高口服生物利用度和抗氧化潜力。SNEDDS 通过在控制条件下混合 Gelucire 44/14、吐温 80 和 PEG 400 来制备。稀释 SNEDDS 的液滴呈球形,尺寸小于 100nm,带中性电荷。非常快的自乳化在 32s 内完成,透光率值超过 99%。最高药物载量为初始载药量的 90.10±0.24%,最高包封效率为 84.20±0.03%。FT-IR 和 DSC 图谱显示成分之间没有相互作用。在缓冲液 pH 值 1.2、4.5 和 6.8 中的溶解度显示出比芹菜素粗粉明显更高的溶解芹菜素。溶解曲线拟合到 Korsmeyer-Peppas 动力学。Caco-2 细胞中的细胞抗氧化活性与无处理相比约为 52.25-54.64%,高于芹菜素粗粉(12.70%)。我们的工作强调了 SNEDDS 提高芹菜素溶解度和通透性并促进抗氧化功效的潜力,这使其很有机会被开发为用于营养保健品的生物活性化合物。
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