通过与聚乙二醇的自发氢键作用实现儿茶素增溶用于干眼症治疗。
Catechin solubilization by spontaneous hydrogen bonding with poly(ethylene glycol) for dry eye therapeutics.
机构信息
Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea.
T2B Infrastructure Center for Ocular Disease, Busan Paik Hospital, Busan, Republic of Korea.
出版信息
J Control Release. 2019 Aug 10;307:413-422. doi: 10.1016/j.jconrel.2019.04.016. Epub 2019 May 20.
Catechin exhibits various pharmacological effects, yet its poor aqueous solubility limits its clinical use. Here, we investigate a facile catechin solubilization method via spontaneous hydrogen bonding between catechin and poly(ethylene glycol) (PEG). The method is extremely simple in that mixing PEG with catechin followed by lyophilization completely converts insoluble catechin to soluble PEG/catechin nanoscale complexes. This solubilized catechin formulation is useful for preparing eyedrop medicine, and we demonstrate that the solubilized catechin exhibits therapeutic effect upon dry eye diseases.
表儿茶素具有多种药理作用，但由于其在水中的溶解度差，限制了其在临床上的应用。在这里，我们通过表儿茶素与聚乙二醇（PEG）之间的自发氢键作用来研究一种简单的表儿茶素增溶方法。该方法非常简单，只需将 PEG 与表儿茶素混合，然后冷冻干燥，即可将不溶性表儿茶素完全转化为可溶性 PEG/表儿茶素纳米级复合物。这种增溶的表儿茶素配方可用于制备眼药水，我们证明增溶的表儿茶素对干眼症具有治疗作用。
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