State Key Laboratory of Bioelectronics, Jiangsu Laboratory for Biomaterials and Devices, School of Biological Science and Medical Engineering, Southeast University, Nanjing, PR China.
Drug Deliv. 2011 Feb;18(2):159-65. doi: 10.3109/10717544.2010.528068. Epub 2010 Oct 28.
Breviscapine lipid emulsions were prepared by a high speed dispersion-homogenization method with optimal formulation and technological method. The proportion of liposomes in breviscapine lipid emulsions, an important character for determining the behavior of drug in vivo belongs to which carriers, was less than 5%. Loading breviscapine into lipid emulsions did increase the breviscapine concentrations in plasma, retarded the clearance, and exhibited the properties of sustained-release concluded by pharmacokinetic parameters: after bolus administration, the elimination phase (t(1/2(β)) = 99.535) of lipid emulsions was 5.4-times longer than that of Injectio Breviscapine. The AUC(0→∞) (14.453-times), k(10) (0.047-times), Cl(s) (0.147-times), and MRT(0→∞) (17.766-times) values also confirmed this trend. The amount of drug in every tissue increased at different levels after intravenous administration of breviscapine lipid emulsions compared with Injectio Breviscapine. The relative exposure value of breviscapine lipid emulsions for plasma and lungs were 29.59 and 5.81, respectively, indicating that the exposure of breviscapine to plasma and lungs was significantly increased by entrapment in lipid emulsions. Other targeting evaluation indexes also proved the superiority of lipid emulsions carrier to deliver drug to the targeting region of vascular and lung diseases therapy.
灯盏花素脂微球通过高速分散-匀化法制备，优化了处方和工艺方法。脂质体在灯盏花素脂微球中的比例（决定药物体内行为的重要特征属于哪种载体）小于 5%。将灯盏花素载入脂微球中确实增加了血浆中的灯盏花素浓度，延缓了清除速度，并通过药代动力学参数表现出缓释特性：静脉推注后，脂微球的消除相（t(1/2(β))=99.535）比灯盏花素注射液长 5.4 倍。AUC(0→∞)（14.453 倍）、k(10)（0.047 倍）、Cl(s)（0.147 倍）和 MRT(0→∞)（17.766 倍）也证实了这一趋势。与灯盏花素注射液相比，静脉注射灯盏花素脂微球后，各组织中的药物量均有不同程度的增加。灯盏花素脂微球在血浆和肺部的相对暴露值分别为 29.59 和 5.81，表明脂质体包封使灯盏花素在血浆和肺部的暴露显著增加。其他靶向评价指标也证明了脂微球载体在将药物递送至血管和肺部疾病治疗的靶向区域方面的优势。
