Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. In some cases, one or more HIF-1 inhibitors are dispersed or encapsulated in a polymeric matrix. In preferred embodiments, the one or more HIF- 1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof for administration. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.
本发明提供了用于输送一种或多种HIF-1
抑制剂的控释剂型制剂。这些控释制剂型制剂包含一种或多种HIF-1
抑制剂与聚合物载体结合或分散。在某些情况下,一种或多种HIF-1
抑制剂分散或封装在聚合物基质中。在优选实施例中,一种或多种HIF-1
抑制剂与聚合物共价结合,形成聚合物-药物共轭物。聚合物载体可以形成成植入物、微粒子、纳米粒子或其组合物以供给药。控释HIF-1制剂提供长效治疗效果,同时通过在长时间内释放低
水平的一种或多种HIF-1
抑制剂和/或HIF-1
抑制剂共轭物来降低副作用。用于输送一种或多种HIF-1
抑制剂的控释剂型制剂可用于治疗或预防与血管化有关的患者疾病或障碍,包括癌症、肥胖症和激素性黄斑病变等眼部疾病。