Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Department of Drug Delivery, Helmholtz Centre for Infection Research (HZI) and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Saarbruecken, Germany.
AAPS PharmSciTech. 2019 Aug 12;20(7):283. doi: 10.1208/s12249-019-1501-1.
A redispersible spray-dried formulation containing curcumin-loaded, lipid-core nanocapsules (LNC-C) was developed for oral administration. The neuroprotective activity of curcumin after the spray-drying process was evaluated in vitro. The spray-dried powder (SD-LNC-C) was produced using a drying adjuvant composed of a blend of maltodextrin and L-leucine (90:10 w/w). Acceptable process yield (~ 70%) and drug content (6.5 ± 0.2 mg g) were obtained. SD-LNC-C was formed by smooth, spherical-shaped particles, and confocal Raman analysis indicated the distribution of the LNC-C on the surface of the leucine/maltodextrin agglomerates. The surface of the agglomerates was formed by a combination of LNC-C and adjuvants, and laser diffraction showed that SD-LNC-C had adequate aqueous redispersion, with no loss of controlled drug release behaviour of LNC-C. The in vitro curcumin activity against the lipopolysaccharide (LPS)-induced proinflammatory response in organotypic hippocampal slice cultures was evaluated. Both formulations (LNC-C and SD-LNC-C) reduced TNF-α to similar levels. Therefore, neuroprotection of curcumin in vitro may be improved by nanoencapsulation followed by spray-drying, with no loss of this superior performance. Hence, the redispersible spray-dried powder proposed here represents a suitable approach for the development of innovative nanomedicines containing curcumin for the prevention/treatment of neurodegenerative diseases.
一种载有姜黄素的可再分散喷雾干燥制剂,即载有姜黄素的脂质核纳米胶囊(LNC-C),被开发用于口服给药。喷雾干燥过程后姜黄素的神经保护活性在体外进行了评估。喷雾干燥粉末(SD-LNC-C)是使用由麦芽糊精和 L-亮氨酸(90:10 w/w)混合物组成的干燥助剂生产的。可获得可接受的工艺收率(约 70%)和药物含量(6.5±0.2 mg g)。SD-LNC-C 由光滑的球形颗粒组成,共焦拉曼分析表明 LNC-C 分布在亮氨酸/麦芽糊精聚集体的表面。聚集体的表面由 LNC-C 和助剂的组合形成,激光衍射表明 SD-LNC-C 具有足够的水相再分散性,没有失去对 LNC-C 控制药物释放行为的影响。在器官型海马切片培养物中,体外姜黄素对脂多糖(LPS)诱导的促炎反应的活性进行了评估。两种制剂(LNC-C 和 SD-LNC-C)均使 TNF-α降低到相似水平。因此,纳米包封后喷雾干燥可提高姜黄素的体外神经保护作用,而不会降低其优异性能。因此,这里提出的可再分散喷雾干燥粉末代表了开发含有姜黄素的新型纳米药物的一种合适方法,用于预防/治疗神经退行性疾病。