Breviscapine (BVP), a flavonoid compound, is widely used in the treatment of cardiovascular and cerebrovascular diseases; however, the low oral bioavailability and short half-life properties limit its application. The aim of this study was to investigate the three preparations for improving its oral bioavailability: nanosuspensions (BVP-NS), liposomes (BVP-LP) and phospholipid complexes (BVP-PLC). In vitro and in vivo results suggested that these three could all significantly improved the cumulative released amount and oral bioavailability compared with physical mixture, in which BVP-PLC was the most optimal preparation with the relative bioavailability and mean retention time of 10.79 ± 0.25 (p < 0.01) and 471.32% (p < 0.01), respectively. Furthermore, the influence of drug-lipid ratios on the in vitro release and pharmacokinetic behavior of BVP-PLC was also studied and the results showed that 1:2 drug-lipid ratio was the most satisfactory one attributed to the moderate-intensity interaction between drug and phospholipid which could balance the drug loading and drug release very well.

中文翻译：

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通过制备纳米混悬剂，脂质体和磷脂复合物提高灯盏花素口服生物利用度

灯盏花素（BVP）是一种类黄酮化合物，被广泛用于治疗心血管和脑血管疾病。但是，口服生物利用度低和半衰期短限制了其应用。这项研究的目的是研究三种改善口服生物利用度的制剂：纳米悬浮液（BVP-NS），脂质体（BVP-LP）和磷脂复合物（BVP-PLC）。体外和体内结果表明，与物理混合物相比，这三种制剂均可显着提高累积释放量和口服生物利用度，其中BVP-PLC是最佳生物制剂，相对生物利用度和平均保留时间为10.79±0.25（p <0.01）和471.32％（p<0.01）。此外，还研究了血脂比对BVP-PLC的体外释放和药代动力学行为的影响，结果表明：1：2的血脂比是最令人满意的，这归因于药物之间的中等强度相互作用磷脂可以很好地平衡载药量和药物释放。