Enhanced solubility and in vitro drug release of diosmetin from soy lecithin based‐diosmetin phytosome

IF 1.3 Q3 CHEMISTRY, MULTIDISCIPLINARY Vietnam Journal of Chemistry Pub Date : 2024-05-14 DOI:10.1002/vjch.202300326
T. Huynh, Bich‐Ngoc Duong, Bao‐Tram Ho, Hoang‐Phuc Nguyen, Anh‐Khoa Ton, Thi‐Cam‐Thu Nguyen, Thi‐Hong‐An Nguyen, Kim‐Khanh‐Huy Ngo, Ngoc‐Kim‐Ngan Phan, Quoc‐Tuan Le, Van‐Thanh Nguyen, Thi‐Kim‐Dung Hoang
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Abstract

The Diosmetin Phytosome (Dt‐Ph) was developed to enhance the complex's aqueous solubility and in vitro drug release compared to pure Diosmetin (Dt). The process variables such as the reactants’ molar ratio, reaction time, stirring speed, and reaction temperature were varied to identify the most appropriate conditions for synthesis. The resulting Dt‐Ph possessed a particle size of 213.9 nm, a zeta potential of −115.1 mV, and a 95.6% encapsulation effectiveness, indicating the successful formation of the phytosome. Scanning electron microscopy (SEM) was used to analyze the morphology of the surface of Dt and Dt‐Ph. The in vitro dissolution in 24 h and normal cell cytotoxic activities of the selected formulation were evaluated. The solubility of Dt‐Ph in buffered media was four times higher than Dt, indicating greater hydrophilicity of Dt‐Ph in comparison to the more lipophilic‐free drug. Additionally, the formulation showed a noticeably increased rate and extent of dissolution studies on drug release, which was two times better than Dt. Cytotoxicity results on HEK‐293A cells showed that Dt‐Ph had less impact on normal cells compared to Dt.
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基于大豆卵磷脂的双香叶酮植物胶囊提高了双香叶酮的溶解度和体外药物释放率
与纯的香叶木素(Dt)相比,开发了香叶木素植物胶囊(Dt-Ph)以提高复合物的水溶性和体外药物释放。通过改变反应物摩尔比、反应时间、搅拌速度和反应温度等工艺变量,确定了最合适的合成条件。最终得到的 Dt-Ph 粒径为 213.9 nm,Zeta 电位为 -115.1 mV,封装效率为 95.6%,表明植物胶体的成功形成。采用扫描电子显微镜(SEM)分析了 Dt 和 Dt-Ph 的表面形态,并对所选制剂的 24 小时体外溶解度和正常细胞的细胞毒活性进行了评估。Dt-Ph 在缓冲介质中的溶解度是 Dt 的四倍,这表明与亲脂性更强的无脂药物相比,Dt-Ph 具有更强的亲水性。此外,在药物释放的溶解研究中,该制剂的溶解速率和溶解度明显提高,是 Dt 的两倍。对 HEK-293A 细胞的细胞毒性结果表明,与 Dt 相比,Dt-Ph 对正常细胞的影响较小。
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来源期刊
Vietnam Journal of Chemistry
Vietnam Journal of Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
1.70
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Pancreatic lipase inhibitory and anti‐acne activity of Piper betle: Kinetic studies, in silico docking, and chemical characterization of bioactive compounds A new cytotoxic saponin from the ethyl acetate extract of Myrsine semiserrata wall Cover Contents: Vietnam Journal of Chemistry 3/2024 Enhanced solubility and in vitro drug release of diosmetin from soy lecithin based‐diosmetin phytosome
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