• 专利标题:   New graphene oxide/reduced graphene oxide-2-methoxyestradiol hybrid used as e.g. anti-cancer drug for treating e.g. skin cancer, has permanent bonding of 2-methoxyestradiol molecules with graphene oxide or reduced graphene oxide.
  • 专利号:   WO2023018342-A1, PL438737-A1
  • 发明人:   GORSKAPONIKOWSKA M, LIPINSKA L, GIERALTOWSKA J, BARAN M, CHLANDA A, KOWIORSKI K, KONIECZNA L, BELKA M, KAMM A, KUBANJANKOWSKA A, GULCZYNSKI J, IZYCKASWIESZEWSKA E, KNAP N, ZOLNIERSKI A, BACZEK T
  • 专利权人:   UNIV GDANSKI MEDYCZNY, SIEC BADAWCZA LUKASIEWICZINST INZYNIERI, NAUK EKONOMICZNYCH PAN INST, UNIV GDANSKI MEDYCZNY, SIEC BADAWCZA LUKASIEWICZINST INZYNIERI, NAUK EKONOMICZNYCH PAN INST
  • 国际专利分类:   A61K031/565, A61K033/44, A61K047/52, A61P035/00, B82Y005/00
  • 专利详细信息:   WO2023018342-A1 16 Feb 2023 A61K-047/52 202321 Pages: 39 English
  • 申请详细信息:   WO2023018342-A1 WOPL050050 12 Aug 2022
  • 优先权号:   PL438737

▎ 摘  要

NOVELTY - A graphene oxide/reduced graphene oxide-2-methoxyestradiol hybrid having a permanent bonding of 2-methoxyestradiol molecules with graphene oxide or reduced graphene oxide, is new. USE - The graphene oxide/reduced graphene oxide-2-methoxyestradiol hybrid is used as anti-cancer drug, and therapeutic system of regulated bioavailability and controller release of active 2-methoxyestradiol substance, for treating skin cancer, preferably malignant melanoma, other cancers of skin and mucous membrane, and cancer of soft tissues and bones, preferably osteosarcoma, and as agent helping process of healing wounds, preferably fungating cancer wounds (all claimed). ADVANTAGE - The graphene oxide/reduced graphene oxide-2-methoxyestradiol hybrid has stable bonding of 2-methoxyestradiol molecules with graphene oxide or reduced graphene oxide, and improved cytotoxic properties against various cancer cells and bioavailability, while minimizing the potential cytotoxicity of graphene nanoplatelets to normotypic cells. The lipophilic structure of the graphene carrier enables more effective interaction between the 2-methoxyestradiol-graphene complex and the lipid membranes, and in consequence more effective penetration into the cells as compared to an isolated 2-methoxyestradiol molecule. DETAILED DESCRIPTION - An INDEPENDENT CLAIM is included for preparation of the graphene oxide/reduced graphene oxide-2-methoxyestradiol hybrid, which involves preparing a graphene oxide or reduced graphene oxide suspension in a concentration of 0.5 mg/ml in dimethyl sulfoxide or 96% ethanol, and a solution of 2-methoxyestradiol in a concentration of 1 mg/ml, instilling the solution of 2-methoxyestradiol into the graphene oxide or reduced graphene oxide suspension in a volume ratio of 1:1, maintaining the reaction mixture for 24 hours at room temperature, centrifuging the reaction mixture for 20 minutes at 1200 rpm, and decanting the supernatant from above the sediment, and washing the sediment with dimethyl sulfoxide or ethanol.