脂质核纳米胶囊是一种替代肺部给药的方法，可提高他汀类药物的稳定性。
Lipid-core nanocapsules are an alternative to the pulmonary delivery and to increase the stability of statins.
机构信息
a Nanoscience Post-Graduation Program , Franciscan University , Santa Maria , Rio Grande do Sul , Brazil.
b Pharmaceutical Sciences Post-Graduation Program , Federal University of Rio Grande do Sul State , Porto Alegre , Brazil.
出版信息
J Microencapsul. 2019 Jun;36(4):317-326. doi: 10.1080/02652048.2019.1624849. Epub 2019 Jun 19.
Lipid-core nanocapsules (LNCs) loaded with simvastatin (SV, SV-LNC) or lovastatin (LV, LV-LNC) were formulated for pulmonary administration. The LNC suspensions were characterized physicochemically, their stability was evaluated, and drug delivery by the pulmonary route was tested . The loaded LNCs had a particle size close to 200 nm, a low polydispersity index, and a zeta potential around -20 mV. The encapsulation efficiency was high for SV (99.21 ± 0.7%) but low for LV (20.34 ± 1.2%). SV release from nanocapsules was slower than it was from SV in solution, with a monoexponential release profile, and the drug emitted and aerosol output rate was higher for SV-LNCs (1.58 µg/s) than for SV in suspension (0.54 µg/s). SV-LNCs had a median aerodynamic diameter of 3.51 µm and a highly respirable fraction (61.9%), indicating that nanoparticles are a suitable system for efficient delivery of simvastatin to the lung.
载有辛伐他汀（SV，SV-LNC）或洛伐他汀（LV，LV-LNC）的脂核纳米胶囊（LNC）被制成用于肺部给药的制剂。对 LNC 混悬液进行了物理化学性质的表征，评估了其稳定性，并测试了通过肺部给药的药物传递情况。载药 LNC 的粒径接近 200nm，多分散指数低，zeta 电位约为-20mV。SV 的包封效率很高（99.21±0.7%），但 LV 较低（20.34±1.2%）。纳米胶囊中 SV 的释放速度比溶液中 SV 慢，呈单指数释放曲线，SV-LNC 的药物释放和气溶胶输出速率（1.58μg/s）比 SV 混悬液（0.54μg/s）更高。SV-LNC 的平均空气动力学直径为 3.51μm，具有高可吸入分数（61.9%），表明纳米颗粒是将辛伐他汀高效递送至肺部的合适系统。
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