Preparation method of drug-loaded microspheres for targeted inhibition of HIF-2alpha, drug-loaded microspheres and applications

• Main Authors: FANG SHIJI, ZHAO ZHONGWEI, CHEN WEIQIAN, DU YONGZHONG, TU JIANFEI, SHU GAOFENG, CHEN MINJIANG, JI JIANSONG
• Format: Patent
• Language: Chinese; English
• Published: 16.11.2021
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention provides a preparation method of a drug-loaded microsphere for targeted inhibition of HIF-2alpha, which is used for preparing the drug-loaded microsphere. The PT-2385 is co-loaded through a microsphere system, an effective sustained-release system of the PT-2385 is formed, the toxic and side effects of the PT-2385 are reduced, meanwhile, the expression of HIF-2alpha can be inhibited in a targeted mode, and the anti-tumor effect of the PT-2385 is improved. Meanwhile, the PT-2385 and adriamycin co-loaded microspheres can achieve a long-term slow release effect in vivo, so that a long-acting anti-tumor effect is achieved. Besides, the novel drug-loaded microspheres jointly loaded with PT-2385 and doxorubicin and used for targeted inhibition of HIF-2alpha are prepared with an emulsion crosslinking method, wherein the glutaraldehyde is used as a crosslinking agent, and hydrochloric acid is used as a catalyst; the method is suitable for batch production of microspheres, and drug-loaded microspheres wi