Polysaccharide from vinegar baked radix bupleuri as efficient solubilizer for water-insoluble drugs of Chinese medicine
Polysaccharide from vinegar baked radix bupleuri as efficient solubilizer for water-insoluble drugs of Chinese medicine
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醋柴胡多糖作为难溶性中药高效增溶剂
DOI：
10.1016/j.carbpol.2019.115473
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发表时间：
2020
影响因子：
11.2
通讯作者：
Zhao Ruizhi
中科院分区：
文献类型：
--
作者：
Zhao Ya;Wan Peng;Wang Jinqiu;Li Ping;Hu Qiaohong;Zhao Ruizhi
开发高效、安全、工艺简单的增溶剂是现代制药工业的重要领域之一。我们先前的研究发现，醋制柴胡多糖(VBCP)是一个潜在的候选成分。本研究旨在阐明VBCP中哪些多糖具有增溶作用及其增溶机理。本文报道了从VBCP中分离得到的一种新型酸性支链多糖VBCP-3-A，它无毒，对黄芩苷和大黄酸具有较高的溶解性。这比吐温80要好得多。其增溶机理可能是VBCP-3-A在水中自组装形成胶束状聚集体，通过氢键和疏水力的相互作用将水不溶性成分包裹起来。体内药动学研究表明，VBCP-3-A提高了黄芩苷和大黄酸的Cmax和AUC(0-t)。这些结果表明，VBCP-3-A是一种高效、安全的潜在增溶剂。
The development of solubilizers with high efficiency, high safety and simple technology is one of the important fields in modern pharmaceutical industry. Our previous study found that vinegar baked Radix Bupleurum polysaccharides (VBCP) was a potential candidate. This study aimed to clarify which polysaccharide in VBCP had solubility enhancement effect and its solubilizing mechanism. Here, we reported that a novel acidic branched polysaccharide from VBCP, VBCP-3-A, which was non-toxic and had high solubility to baicalin and rhein. It was much better than that of Tween 80. The solubilization mechanism might be that VBCP-3-A self-assembled to form micelle-like aggregates in water, which can encapsulate water-insoluble constituents through the interaction of both hydrogen bonding and hydrophobic forces.in vivopharmacokinetic study showed that VBCP-3-A increased Cmaxand AUC(0-t)of baicalin and rhein. Those results suggested that VBCP-3-A was a potential solubilizer with high efficiency and high safety.