Michalowski Cecilia B, Arbo Marcelo D, Altknecht Louise, Anciuti Andréia N, Abreu Angélica S G, Alencar Luciana M R, Pohlmann Adriana R, Garcia Solange C, Guterres Sílvia S
Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, Brazil.
Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegre 90610-000, Brazil.
Pharmaceutics. 2020 Jan 18;12(1):80. doi: 10.3390/pharmaceutics12010080.
Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate dispersity (laser diffraction and dynamic light scattering). Zeta potential was inverted from -14.3 mV [LNC-Fur(0,5)] to +18.3 mV after chitosan coating. Transmission electron microscopy and atomic force microscopy showed spherical structures corroborating the nanometric diameter of the nanocapsules. Regarding the systolic pressure, on the first day, the formulations showed antihypertensive effect and a longer effect than the respective drug solutions. When both drugs were associated, the anti-hypertensive effect was prolonged. On the fifth day, a time effect reduction was observed for all treatments, except for the nanocapsule formulation containing both drugs [Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]. For diastolic pressure, only Capt(0.5)-Zn(25)-MLNC-Fur(0.45) presented a significant difference ( < 0.05) on the first day. On the fifth day, both Capt(0.5)-MLNC-Fur(0.45) and Capt(0.5)-Zn(25)-MLNC-Fur(0.45) had an effect lasting up to 24 h. The analysis of early kidney damage marker showed a potential protection in renal function by Capt(0.5)-Zn(25)-MLNC-Fur(0.45). In conclusion, the formulation Capt(0.5)-Zn(25)-MLNC-Fur(0.45) proved to be suitable for hypertension treatment envisaging an important innovation.
开发了一种用卡托普利功能化且在核心中纳米包封速尿的多壁脂质核纳米胶囊（MLNC）作为口服液体制剂。这些纳米胶囊的平均粒径低于200nm，呈现单峰且窄的粒径分布以及中等分散度（激光衍射和动态光散射）。壳聚糖包衣后，zeta电位从-14.3mV[LNC-Fur(0,5)]变为+18.3mV。透射电子显微镜和原子力显微镜显示出球形结构，证实了纳米胶囊的纳米级直径。关于收缩压，在第一天，这些制剂显示出降压作用，且作用时间比各自的药物溶液更长。当两种药物联合使用时，降压作用得以延长。在第五天，除了含有两种药物的纳米胶囊制剂[Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]外，所有处理均观察到时间效应降低。对于舒张压，仅Capt(0.5)-Zn(25)-MLNC-Fur(0.45)在第一天呈现出显著差异（<0.05）。在第五天，Capt(0.5)-MLNC-Fur(0.45)和Capt(0.5)-Zn(25)-MLNC-Fur(0.45)的作用均持续长达24小时。早期肾损伤标志物分析表明，Capt(0.5)-Zn(25)-MLNC-Fur(0.45)对肾功能具有潜在保护作用。总之，制剂Capt(0.5)-Zn(25)-MLNC-Fur(0.45)被证明适用于高血压治疗，这是一项重要的创新。
