Song Zilin, Yin Jiaojiao, Xiao Peifu, Chen Jin, Gou Jingxin, Wang Yanjiao, Zhang Yu, Yin Tian, Tang Xing, He Haibing
Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of Food and Wine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
Pharmaceutics. 2021 Jan 20;13(2):132. doi: 10.3390/pharmaceutics13020132.
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 ( < 0.01) and 471.32% ( < 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.
灯盏花素（BVP）是一种黄酮类化合物，广泛应用于心血管和脑血管疾病的治疗；然而，其低口服生物利用度和短半衰期特性限制了它的应用。本研究的目的是研究三种提高其口服生物利用度的制剂：纳米混悬液（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，这三种制剂均能显著提高累积释放量和口服生物利用度，其中BVP-PLC是最优化的制剂，相对生物利用度和平均滞留时间分别为10.79±0.25（<0.01）和471.32%（<0.01）。此外，还研究了药物-脂质比对BVP-PLC体外释放和药代动力学行为的影响，结果表明，药物-脂质比为1:2时最令人满意，这归因于药物与磷脂之间的中等强度相互作用，能够很好地平衡药物负载和药物释放。
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