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    • 26. 发明公开
    • HYALURONIC ACID-BASED AMPHIPHILIC POLYMER, PREPARATION METHOD AND APPLICATION THEREOF
    • 透明质酸基两性聚合物及其制备方法和应用
    • EP3241852A1
    • 2017-11-08
    • EP16734888.7
    • 2016-01-04
    • BrightGene Bio-Medical Technology Co., Ltd.
    • ZHONG, ZhiyuanZHONG, YinanMENG, FenghuaYUAN, JiandongHUANG, YangqingCHI, Jianwen
    • C08B37/08A61K47/36A61P35/00A61K9/51
    • A61K9/5161A61K9/51A61K31/704A61K31/728A61K31/795A61K47/183A61K47/20A61K47/36C08B37/0072
    • Disclosed are a hyaluronic acid-based amphiphilic polymer, preparation method and application thereof. A main chain of the amphiphilic polymer is a hydrophilic hyaluronic acid and can be employed in active targeting, and a side chain thereof is a hydrophobic group represented by Formula (1). The amphiphilic polymer can carry a small molecule anticancer drug. Polymer nanoparticles are obtained via chemical crosslinking, such that the nanoparticles are not readily dissociated outside a cell or in blood, thus ensuring the stability of a drug encapsulated by the nanoparticles. Upon arriving at a tumor tissue, the hyaluronic acid on a surface of the nanoparticle can immediately combine with a CD44 receptor on a surface of a tumor cell, and effectively enter the tumor cell via endocytosis mediated by the receptor, and then quickly de-crosslink to be dissociated. The drug is quickly released, obtaining an enrichment ratio at a tumor site markedly higher than that of the prior art, resulting in a highly effective treatment, and addressing deficiencies such as drug leakage, low carrying efficiency, low occurrence of endocytosis and slow release in a cell.
    • 公开了一种基于透明质酸的两亲聚合物及其制备方法和应用。 两亲性聚合物的主链是亲水性透明质酸,可以用于主动靶向,其侧链是由式(1)表示的疏水性基团。 两亲聚合物可以携带小分子抗癌药物。 通过化学交联获得聚合物纳米颗粒,使得纳米颗粒不容易在细胞外或血液中解离,从而确保纳米颗粒包封的药物的稳定性。 当到达肿瘤组织时,纳米颗粒表面上的透明质酸可以立即与肿瘤细胞表面上的CD44受体结合,并且通过受体介导的内吞作用有效地进入肿瘤细胞,然后快速地解交联 被分离。 药物迅速释放,获得比现有技术显着更高的肿瘤部位的富集比率,得到高度有效的治疗,并且解决了诸如药物泄漏,携带效率低,内吞作用发生率低以及缓慢释放 一个小区。