Diedrich Camila, Zittlau Isabella C, Khalil Najeh M, Leontowich Adam F G, Freitas Rilton A de, Badea Ildiko, Mainardes Rubiana M
Pharmaceutical Nanotechnology Laboratory, Universidade Estadual do Centro-Oeste, Guarapuava 85040-167, Brazil.
Canadian Light Source, Saskatoon, SK S7N 2V3, Canada.
Pharmaceutics. 2023 May 25;15(6):1592. doi: 10.3390/pharmaceutics15061592.
Luteolin (LUT) is a flavonoid found in several edible and medicinal plants. It is recognized for its biological activities such as antioxidant, anti-inflammatory, neuroprotective, and antitumor effects. However, the limited water solubility of LUT leads to poor absorption after oral administration. Nanoencapsulation may improve the solubility of LUT. Nanoemulsions (NE) were selected for the encapsulation of LUT due to their biodegradability, stability, and ability to control drug release. In this work, chitosan (Ch)-based NE was developed to encapsulate luteolin (NECh-LUT). A 2 factorial design was built to obtain a formulation with optimized amounts of oil, water, and surfactants. NECh-LUT showed a mean diameter of 67.5 nm, polydispersity index 0.174, zeta potential of +12.8 mV, and encapsulation efficiency of 85.49%. Transmission electron microscopy revealed spherical shape and rheological analysis verified the Newtonian behavior of NECh-LUT. SAXS technique confirmed the bimodal characteristic of NECh-LUT, while stability analysis confirmed NECh-LUT stability when stored at room temperature for up to 30 days. Finally, in vitro release studies showed LUT controlled release up to 72 h, indicating the promising potential of NECh-LUT to be used as novel therapeutic option to treat several disorders.
木犀草素（LUT）是一种存在于多种可食用和药用植物中的黄酮类化合物。它因其抗氧化、抗炎、神经保护和抗肿瘤等生物活性而闻名。然而，LUT的水溶性有限，导致口服后吸收不佳。纳米包封可能会改善LUT的溶解度。由于纳米乳液（NE）具有生物可降解性、稳定性和控制药物释放的能力，因此被选择用于包封LUT。在这项工作中，开发了基于壳聚糖（Ch）的NE来包封木犀草素（NECh-LUT）。构建了一个二因素设计，以获得具有优化的油、水和表面活性剂用量的配方。NECh-LUT的平均直径为67.5nm，多分散指数为0.174，zeta电位为+12.8mV，包封效率为85.49%。透射电子显微镜显示为球形，流变学分析证实了NECh-LUT的牛顿流体行为。小角X射线散射技术证实了NECh-LUT的双峰特性，而稳定性分析证实了NECh-LUT在室温下储存长达30天时的稳定性。最后，体外释放研究表明LUT可控制释放长达72小时，表明NECh-LUT作为治疗多种疾病的新型治疗选择具有广阔的应用前景。
