• 专利标题:   Targeted medicine-loaded nanomicelle useful in e.g. preparing cancer medicines preferably an active medicine for inhibiting cancer, inhibiting cancer activity associated with cancer cells or cancer tissues that express.
  • 专利号:   CN112274654-A, CN112274654-B
  • 发明人:   WANG C, ZHENG Y, FANG X, YANG Y
  • 专利权人:   NAT CENT NANOSCIENCE TECHNOLOGY CHINA
  • 国际专利分类:   A61K031/704, A61K045/00, A61K047/10, A61K047/26, A61K047/64, A61K047/69, A61K009/19, A61P035/00, B82Y040/00, B82Y005/00
  • 专利详细信息:   CN112274654-A 29 Jan 2021 A61K-047/69 202115 Pages: 18 Chinese
  • 申请详细信息:   CN112274654-A CN11281084 16 Nov 2020
  • 优先权号:   CN11281084

▎ 摘  要

NOVELTY - Targeted medicine-loaded nanomicelle i.e., a nanomicelle with a cancer-targeting polypeptide covalently attached to the surface and encapsulating a chemotherapeutic medicine, is claimed. The cancer-targeting polypeptide is a polypeptide capable of targeted binding to cancer cells or cancer tissues that express or overexpress the CD36 protein receptor. The particle size of the targeted medicine-loaded nanomicelles is 10-100 nm, more preferably 10-50 nm, and further preferably 20-50 nm. USE - The targeted medicine-loaded nanomicelles are useful in preparing cancer medicines preferably an active medicine for inhibiting cancer, the medicine is a medicine that inhibits cancer activity associated with cancer cells or cancer tissues that express or overexpress the protein receptor CD36, more preferably, the cancer associated with cancer cells or cancer tissues that express or overexpress the protein receptor CD36 comprising glioma, leukemia, oral cancer, liver cancer, preferably, leukemia or liver cancer (claimed). ADVANTAGE - The medicine -loaded micelle increases the drug-loading amount of the micelle, improves the biological stability of the polypeptide and the small molecule chemotherapeutic drug, and increases the targeted binding of the anti-cancer drug in cancer cells and recognition ability and chemotherapeutic drug, and improves cancer treatment effect. DETAILED DESCRIPTION - INDEPENDENT CLAIMS are also included for: preparing the targeting medicine-loaded nanometre micelle comprising (i) respectively preparing micelle molecule solution, micelle molecule solution covalently connected with cancer targeting polypeptide and chemotherapeutic medicine molecule solution, where the micelle molecule solution of the covalently linked cancer targeting polypeptide is obtained by chemical coupling of a maleimide group-modified micelle molecule and a cancer-targeting polypeptide molecule having a Cterminal thiol-SH-containing group, (ii) mixing the three solutions obtained in the step (i) uniformly, steaming, hydrating, allowing to stand, obtaining the target medicine-loaded nano-micelle, and (iii) sterilizing the target medicine carrying nanometre micelle solution obtained in the step (ii), preferably, the solution of step (ii) is filtered by a 0.22 mu filter membrane; and medicine comprising the targeted medicine-loaded nanomicelles, preferably, the dosage form is a lyophilized agent including mannitol, sucrose, and lactose, preferably mannitol.