College of Pharmacy, Guangxi University of Chinese Medicine.
Key Laboratory of Common Technology of Chinese Medicine Preparations, Guangxi University of Chinese Medicine.
Biol Pharm Bull. 2022 Aug 1;45(8):1106-1115. doi: 10.1248/bpb.b22-00154. Epub 2022 May 20.
Andrographolide (AG), a natural product with various pharmacological effects, exhibited low oral bioavailability owing to its poor solubility, stability, and low absorption. Previous studies have suggested that phospholipid (PC) and hydroxypropyl-β-cyclodextrin (HPCD) could improve the drug solubility and absorption. Moreover, nanoemulsion (NE) has been confirmed as an appropriate enhancer for oral bioavailability. Therefore, AG/HPCD/PC complex (AHPC) was synthesized, and AHPC-loaded nanoemulsion (AHPC-NE) was optimized and prepared using central composite design combined response surface methodology. The average droplet size and polydispersity index (PDI) were 116.50 ± 5.99 and 0.29 ± 0.03 nm, respectively. AHPC-NE with a loading capacity of 0.32 ± 0.01% and an encapsulation efficiency of 96.43 ± 2.27% appeared round and uniformly dispersed based on transmission electron microscopy. In vivo release studies demonstrated that AHPC-NE had good sustained-release effects. Further, AHPC-NE significantly enhanced the absorption of AG with a relative bioavailability of 550.71% compared to AG suspension. Such findings reveal AHPC-NE as a potential strategy for sustained-release and oral bioavailability enhancement.
穿心莲内酯（AG）是一种具有多种药理作用的天然产物，由于其溶解度、稳定性和吸收率低，口服生物利用度较低。先前的研究表明，磷脂（PC）和羟丙基-β-环糊精（HPCD）可以提高药物的溶解度和吸收。此外，纳米乳（NE）已被证实是提高口服生物利用度的合适增强剂。因此，合成了 AG/HPCD/PC 复合物（AHPC），并采用中心复合设计结合响应面法优化并制备了 AHPC 负载的纳米乳（AHPC-NE）。平均粒径和多分散指数（PDI）分别为 116.50±5.99nm 和 0.29±0.03nm。基于透射电子显微镜，载药量为 0.32±0.01%、包封率为 96.43±2.27%的 AHPC-NE 呈圆形且均匀分散。体内释放研究表明，AHPC-NE 具有良好的缓释效果。此外，与 AG 混悬液相比，AHPC-NE 显著提高了 AG 的吸收，相对生物利用度为 550.71%。这些发现表明 AHPC-NE 是一种提高缓释和口服生物利用度的潜在策略。
