公开(公告)号：US20160243189A1

公开(公告)日：2016-08-25

申请号：US15142709

申请日：2016-04-29

Applicant: UNIVERSITY OF WATERLOO

Inventor： Frank Xiaofei GU ,  Shengyan LIU ,  Lyndon William James JONES

IPC: A61K38/13 ,  A61K9/00 ,  A61K9/16

CPC classification number: A61K38/13 ,  A61K9/0048 ,  A61K9/006 ,  A61K9/1647 ,  A61K9/5123 ,  A61K9/5153 ,  A61K9/5161 ,  A61K9/5192 ,  A61K31/131 ,  A61K31/69 ,  A61K31/78 ,  A61K45/06 ,  A61K47/26 ,  A61K47/54 ,  A61K47/549 ,  A61K47/6935 ,  A61K47/6937 ,  A61K47/6939 ,  A61K49/0002 ,  Y10T428/2982

Abstract: Disclosed is a mucoadhesive nanoparticle delivery system for delivering an immunosuppressant, such as cyclosporine A, to a mucosal site for treatment of a disease or condition involving inflammation or excess immune activity. The system comprises nanoparticles formed from a plurality of linear amphiphilic block copolymers, each having a hydrophobic block comprising polylactide (PLA) and a hydrophilic block comprising dextran. The nanoparticles are surface-functionalized with a mucosal targeting moiety, such as a phenylboronic acid derivative, for targeted delivery and enhanced retention at the mucosal site. Pharmaceutical compositions, methods, and uses thereof comprising the mucoadhesive nanoparticle delivery system are disclosed. The compositions can be administered in an effective amount for treating the disease or condition while substantially preserving or restoring the function and/or integrity of the mucosal lining. The composition may be formulated as an aqueous suspension for administration to an anterior surface of the eye in the treatment of dry eye syndrome.

Abstract translation: 公开了一种用于将免疫抑制剂如环孢霉素A递送至粘膜部位的粘膜粘附纳米颗粒递送系统，用于治疗涉及炎症或过量免疫活性的疾病或病症。 该系统包含由多个线性两亲嵌段共聚物形成的纳米颗粒，每个嵌段共聚物均具有包含聚丙交酯（PLA）的疏水嵌段和包含葡聚糖的亲水嵌段。 纳米颗粒用粘膜靶向部分如苯基硼酸衍生物进行表面官能化，用于靶向递送，并增强粘膜部位的保留。 公开了包含粘膜粘附纳米颗粒递送系统的药物组合物，方法和用途。 组合物可以以有效量施用以治疗疾病或病症，同时基本上保留或恢复粘膜内层的功能和/或完整性。 组合物可以配制成水性悬浮液，用于在干眼综合征的治疗中给予眼前表面。