Tecnológico Nacional de México / I.T.Tepic, Laboratorio Integral de Investigación en Alimentos, Avenida Instituto Tecnológico No. 2595, Lagos del Country CP 63175, Tepic, Nayarit, México.
Instituto de Farmacobiología, Universidad de la Cañada, Teotitlán-San Antonio Nanahuatipán st., Km 1.7, Paraje Titlacuatitla, CP 68540, Teotitlán de Flores Magón, Oaxaca, México.
Anticancer Agents Med Chem. 2023;23(10):1174-1183. doi: 10.2174/1871520622666220617101515.
Lupeol (LP) and Mangiferin (MG) have beneficial effects on health. However, their pharmacokinetic properties can affect their bioavailability when administered orally. Therefore, their incorporation as a vehicle in a hybrid matrix of ZnO and PLGA could contribute to improving bioavailability.
This study aimed to develop this matrix and evaluate the optical and bioactive properties obtained by the solvent emulsion and evaporation methods. These were subjected to processes to evaluate their bioactivity in relation with topoisomerase.
Functionalized treatment number 15 (T15) showed the best results in studies of controlled release and encapsulation efficiency of lupeol (LP) and mangiferin (MG) (60.01 ± 1.24% and 57.71 ± 1.94%). The best treatment showed behavior as a topoisomerase II inhibitor (18.60 ± 1.55). The nanoparticles developed in this study did not show a cytotoxic effect on BEAS-2B, while HepG2, showed a decrease in viability (IC50 1549.96 ± 174.62 μg/mL). However, although the hemolytic activity is not shown after 1 h of exposure, morphological alterations caused by T15 are observed at concentrations of 2500 and 1250 μg/mL.
The TF15 treatment shown maintaining antitopoisomerasa activity does and does not cytotoxixity for healthy cells and slows down the growth of cancer cells.
羽扇豆醇（LP）和芒果苷（MG）对健康有益。然而，当口服给药时，它们的药代动力学特性会影响其生物利用度。因此，将它们作为载体掺入 ZnO 和 PLGA 的混合基质中可以有助于提高生物利用度。
本研究旨在开发这种基质，并通过溶剂乳化和蒸发方法评估获得的光学和生物活性特性。对它们进行了与拓扑异构酶相关的生物活性评估过程。
功能化处理 15 号（T15）在羽扇豆醇（LP）和芒果苷（MG）的控制释放和包封效率研究中显示出最佳结果（60.01±1.24%和 57.71±1.94%）。最佳处理表现出拓扑异构酶 II 抑制剂的行为（18.60±1.55）。本研究开发的纳米粒子对 BEAS-2B 没有显示出细胞毒性作用，而 HepG2 显示出活力下降（IC50 为 1549.96±174.62μg/mL）。然而，尽管在暴露 1 小时后没有显示出溶血活性，但在 2500 和 1250μg/mL 浓度下观察到 T15 引起的形态改变。
TF15 处理显示保持抗拓扑异构酶活性，对健康细胞无细胞毒性，并减缓癌细胞的生长。
