Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Andrographolide/Phospholipid/Cyclodextrin Complex-Loaded Nanoemulsion: Preparation, Optimization, in Vitro and in Vivo Evaluation
Linghui ZouWenya DingQiuyan HuangXu YangJilang LiTianyan HuangZeyu LiSi LinJianfang Feng
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2022 Volume 45 Issue 8 Pages 1106-1115


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.

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© 2022 The Pharmaceutical Society of Japan
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