公开(公告)号：WO2015169849A1

公开(公告)日：2015-11-12

申请号：PCT/EP2015/059941

申请日：2015-05-06

申请人： NEMYSIS LIMITED

发明人： PITARRESI, Giovanna ,  PALUMBO, Fabio Salvatore ,  GIAMMONA, Gaetano

IPC分类号： A61K47/36 ,  A61K9/19 ,  A61K9/20 ,  C08B37/08 ,  A61K38/43

CPC分类号： A61K47/36 ,  A61K9/0053 ,  A61K9/06 ,  A61K9/19 ,  A61K9/205 ,  A61K38/482 ,  A61K47/14 ,  A61K47/18 ,  A61K47/26 ,  C08B37/0072 ,  C08J3/24 ,  C08J3/28 ,  C08J2305/08 ,  C08L5/08 ,  C12Y304/21026

摘要： The present invention relates to a composition comprising hydrogels from functionalized hyaluronic acid derivatives, said hydrogels loaded with exogenous enzymes selected in the group consisting of prolyl endopeptidase (PEP) and endoprotease (EP)intended for the oral treatment of celiac disease. Specifically, this invention concerns a one-pot methodology useful to prepare methacrylic derivatives of hyaluronic acid, through the formation of a specific active group on hydroxyl groups of hyaluronic acid, the subsequent substitution of the inserted active group with ethylenediamine and finally, the reaction with methacrylic anhydride. The obtained methacrylic hyaluronic acid derivatives are used to prepare hydrogels through irradiation and loaded with exogenous enzymes selected in the group consisting of prolyl endopeptidase (PEP) and endoprotease (EP). The ability of prepared hydrogels to allow the enzyme release, as active form in simulated gastrointestinal fluids is proved.

摘要翻译： 本发明涉及包含来自官能化透明质酸衍生物的水凝胶的组合物，所述水凝胶装载有选自用于口腔治疗乳糜泻的脯氨酰内肽酶（PEP）和内切蛋白酶（EP）的外源性酶。 具体而言，本发明涉及通过在透明质酸的羟基上形成特定的活性基团，随后用乙二胺替代插入的活性基团，最后与...的反应，可用于制备透明质酸的甲基丙烯酸衍生物的一锅法 甲基丙烯酸酐。 所得甲基透明质酸衍生物用于通过照射制备水凝胶并加载选自脯氨酰内肽酶（PEP）和内切蛋白酶（EP）的外源酶。 证明了制备的水凝胶允许酶释放作为模拟胃肠液中活性形式的能力。