申请人:THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
公开号:US20160361425A1
公开(公告)日:2016-12-15
Methods for modifying therapeutic agents such as therapeutic biomolecules, such as proteins for improved oral, rectal or transmucosal delivery, as well as compositions made using such methods and methods of administering such compositions to a subject, are disclosed. Specifically, the therapeutic agents are conjugated to hyperbranched polymers (HBPs), such as hyperbranched polyglycerol (HPG). When such conjugates are administered orally to a subject, the HBP protects the therapeutic agent from the acid environment of the stomach and protease attack in the gastro-intestinal tract, while facilitating the absorption of the therapeutic agent in the higher pH environment of the intestines. The methods and compositions are useful for the improved administration of a variety of therapeutic agents to a subject.
本发明涉及改进口服、直肠或黏膜透传输的治疗生物分子(例如蛋白质)的方法,以及使用这些方法制备的组合物和将这些组合物用于治疗的方法。具体而言,本发明将治疗生物分子与高分支聚合物(HBPs)如高分支聚甘油(HPG)共轭。当这种共轭物被口服给予受试者时,HBP可以保护治疗生物分子免受胃酸环境和胃肠道的蛋白酶攻击,同时促进治疗生物分子在肠道更高的pH环境中的吸收。这些方法和组合物可用于改善给予受试者各种治疗生物分子的途径。