Abstract Ginkgolide B (GB) and Puerarin (Pue) are active pharmaceutical ingredients for the treatment of Parkinson’s disease (PD); however, both are poorly water-soluble, which limits their bioavailability. The present study used the niosome vesicle encapsulation technique to prepare a novel GB composite drug. The conditions for GB–Pue niosomal complex preparation were as follows: a hydration temperature of 60°C, a hydrophilic–lipophilic balance of 10.5, a drug–carrier mass ratio of 8:100, and a surfactant–cholesterol mass ratio of 1.5:1. The niosomal complex suspension was uniformly distributed and milky white in color, with no stratification over a duration of 1 month. It had an average particle size of 187.3 nm, a particle-size distribution of 0.237, a GB encapsulation efficiency (EE) of 68.2%, a GB drug-loading rate of 90.1%, a Pue EE of 40.5%, and a Pue drug-loading rate of 83.3%. The optimal storage temperature for the niosomal complex suspension was 4°C. Following an intravenous injection of the niosomal complex suspension into the rat tail, the area under the curve (AUC) from 0 to 4 h was 54.1 h µg mL−1, with a mean residence time (MRT) of 0.96 h, a distribution half-life (T 1/2α) of 0.195 h, and a total clearance of 0.003 L h−1 kg−1. The AUC and MRT of the composite prescription were 1.1- and 1.4-times those of the commercial injection, respectively, showing significantly increased sustained release and bioavailability. Moreover, the distribution of GB in the brain tissue was 1.8-times that of the commercial injection. In conclusion, the novel GB niosomal composite drug, with excellent stability, improved pharmacokinetics, and brain tissue distribution, demonstrates great potential for the delivery of GB and Pue for PD therapeutics.

中文翻译：

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一种新型银杏内酯B脂质体复合药物的制备

摘要 银杏内酯B（GB）和葛根素（Pue）是治疗帕金森病（PD）的活性药物成分；然而，两者都难溶于水，这限制了它们的生物利用度。本研究采用 niosome 囊泡封装技术制备了一种新型 GB 复合药物。GB-Pue 脂质体复合物制备条件如下：水合温度为 60°C，亲水亲油平衡为 10.5，药物载体质量比为 8:100，表面活性剂与胆固醇质量比为 1.5： 1. Niosomal 复合物悬浮液分布均匀，呈乳白色，在 1 个月内没有分层。平均粒径187.3 nm，粒径分布0.237，GB包封率（EE）68.2%，GB载药率90.1%，Pue EE 40.5%，和83.3%的Pue载药率。Niosomal 复合物悬浮液的最佳储存温度为 4°C。将 niosomal 复合物混悬液静脉注射到大鼠尾后，0 到 4 小时的曲线下面积 (AUC) 为 54.1 h µg mL-1，平均停留时间 (MRT) 为 0.96 h，分布的一半- 寿命 (T 1/2α) 为 0.195 小时，总间隙为 0.003 L h-1 kg-1。复合处方的 AUC 和 MRT 分别是商业注射剂的 1.1 倍和 1.4 倍，显示出显着增加的缓释和生物利用度。此外，GB在脑组织中的分布是商业注射剂的1.8倍。综上所述，新型GB niosomal 复合药物，具有优异的稳定性、改善的药代动力学和脑组织分布，