Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, Pavas, San José 1174-1200, Costa Rica.
Laboratorio BIODESS, Escuela de Química, Universidad de Costa Rica, San Pedro de Montes de Oca, San José 2060, Costa Rica.
Molecules. 2022 Apr 25;27(9):2758. doi: 10.3390/molecules27092758.
Bovine Serum Albumin (BSA) lipid hybrid nanoparticles are part of the new solutions to overcome low bioavailability of poor solubility drugs such as curcuminoids, which possess multiple biological advantages; however, they are counterbalanced by its short biological half-life. In this line, we prepared the three main curcuminoids: curcumin (CUR), desmethoxycurcumin (DMC), and bisdemethoxycurcumin (BDM)-loaded BSA nanoparticles. The three formulations were characterized by the average size, size distribution, crystallinity, weight loss, drug release, kinetic mechanism, and antioxidant activity. The developed method produced CUR-, DMC-, and BDM-loaded BSA nanoparticles with a size average of 15.83 ± 0.18, 17.29 ± 3.34, and 15.14 ± 0.14 nm for CUR, DMC, and BDM loaded BSA, respectively. FT-IR analysis confirmed the encapsulation, and TEM images showed their spherical shape. The three formulations achieved encapsulation efficiency upper to 96% and an exhibited significantly increased release from the nanoparticle compared to free compounds in water. The antioxidant activity was enhanced as well, in agreement with the improvement in water release, obtaining IC values of 9.28, 11.70, and 15.19 µg/mL for CUR, DMC, and BDM loaded BSA nanoparticles, respectively, while free curcuminoids exhibited considerably lower antioxidant values in aqueous solution. Hence, this study shows promises for such hybrid systems, which have been ignored so far, regarding proper encapsulation, protection, and delivery of curcuminoids for the development of functional foods and pharmaceuticals.
牛血清白蛋白(BSA)脂质杂化纳米粒是克服低生物利用度的新型解决方案的一部分,这些解决方案适用于溶解度差的药物,如姜黄素类,它们具有多种生物学优势;然而,其短的生物半衰期也对其产生了影响。在这一方面,我们制备了三种主要的姜黄素类化合物:姜黄素(CUR)、脱甲氧基姜黄素(DMC)和双脱甲氧基姜黄素(BDM)负载的 BSA 纳米粒。这三种制剂的平均粒径、粒径分布、结晶度、失重、药物释放、动力学机制和抗氧化活性均通过特征得以体现。所开发的方法可制备 CUR、DMC 和 BDM 负载的 BSA 纳米粒,其平均粒径分别为 15.83 ± 0.18nm、17.29 ± 3.34nm 和 15.14 ± 0.14nm。FT-IR 分析证实了包封,TEM 图像显示其为球形。这三种制剂的包封效率均高于 96%,与游离化合物在水中相比,纳米粒的释放明显增加。抗氧化活性也得到了增强,与水释放的改善一致,CUR、DMC 和 BDM 负载的 BSA 纳米粒的 IC 值分别为 9.28、11.70 和 15.19μg/mL,而游离姜黄素类化合物在水溶液中的抗氧化值要低得多。因此,这项研究表明,对于目前被忽视的此类杂化系统,在适当的封装、保护和递送姜黄素类化合物以开发功能性食品和药物方面具有广阔的前景。