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SILICON PARTICLES TARGETING TUMOR CELLSCM Patents

A silicon particle comprising a silicon body, a functionalized silica surface surrounding the silicon body, and a targeting moiety specifically targeting tumor cells, and, optionally, an enzymatically metabolizable compound, is useful in the treatment of cancer by producing cell death after particle internalization.

Datos clave

CategoríaInvención

Índice de la ficha

Updated at
05/11/2026
Numero publicacion
EP.2946793.A1
Fecha publicacion
25/11/2015
Anio publicacion
2015
Numero solicitud
EP20140382182

En detalle

Reivindicaciones

1. A silicon particle selected from the group consisting of a type I silicon particle and a type II silicon particle, wherein the type I silicon particle comprises: a. a silicon body, b. a silica surface surrounding the silicon body, wherein the silica surface is functionalized by at least one functional group, and wherein said functional group is capable of setting up a bond with an enzymatically metabolizable compound, c. an enzymatically metabolizable compound, wherein said compound is linked to (i) said silica surface through said functional group and to (ii) a targeting moiety, and d. a targeting moiety, wherein said moiety is linked to the particle through said enzymatically metabolizable compound, and wherein the type II silicon particle comprises: a. a silicon body, b. a silica surface surrounding the silicon body, wherein the silica surface is functionalized by at least one functional group, and wherein said functional group is capable of setting up a bond with a targeting moiety, and c. a targeting moiety, wherein said moiety is directly linked to said functionalized silica surface. 2. The particle according to claim 1, wherein said silica surface is functionalized by reaction with a compound selected from the group comprising an halosilane, an organosilane, a silanol, a siloxane, an aminosilane, a mercaptosilane and a glycidoxysilane. 3. The particle according to claim 1 or 2, wherein said silica surface is functionalized by reaction with aminopropylsilane (APS). 4. The particle according to any one of claims 1 to 3, wherein said enzymatically metabolizable compound is selected from the group comprising a carbohydrate, a lipid, a peptide, a protein and a nucleic acid. 5. The particle according to claim 4, wherein said enzymatically metabolizable carbohydrate is a glucopyranoside. 6. The particle according to any one of claims 1 to 5, wherein said targeting moiety is a molecule able to specifically recognize and bind to a cell receptor of a target cell, wherein said targeting moiety is selected from the group comprising an antibody or an antigen binding fragment thereof, a binding structure, an aptamer, a peptide or a small molecule. 7. A process for the preparation of a particle according to any of claims 1 to 6, selected from the group consisting of "Process I" and "Process II", - wherein Process I comprises: i) contacting a silicon particle comprising a silicon body and a functionalized silica surface with an enzymatically metabolizable compound under conditions suitable for binding the compound to the functionalized silica surface; and ii) contacting the product resulting from step i) with a targeting moiety under conditions suitable for binding the targeting moiety to the compound bound to the functionalized silica surface, and - wherein Process II comprises contacting a silicon particle comprising a silicon body and a functionalized silica surface with a targeting moiety under conditions suitable for binding the targeting moiety to the functionalized silica surface. 8. A composition comprising at least a particle according to any of claims 1 to 6 and a suitable medium. 9. A pharmaceutical composition comprising a therapeutically effective amount of a particle according to any of claims 1 to 6 and a pharmaceutically acceptable excipient. 10. The pharmaceutical composition according to claim 9, which further comprises an anti-cancer agent. 11. The particle according to any of claims 1 to 6, or the pharmaceutical composition according to claim 9 or 10, for use in medicine. 12. The particle according to any of claims 1 to 6 for use in the prevention and/or treatment of cancer. 13. The particle for use according to claim 12, wherein prevention and/or treatment of cancer comprises killing tumor cells. 14. The particle for use according to claim 12 or 13, wherein the cancer is selected from the group consisting of breast cancer, colon cancer, gastric cancer, lung cancer, gall bladder cancer, colorectal cancer, bone cancer, sarcoma, esophageal cancer, head and neck carcinomas, ovarian cancer, prostate cancer, liver cancer, melanoma, glioma and neuroblastoma.

Etiquetas

Inventores
Álvarez Puebla, Ramón ÁngelÁlvarez Puebla Ramón ÁngelFenollosa Esteve RobertoFenollosa Esteve, RobertoMesseguer Rico, Francisco JavierMesseguer Rico Francisco JavierRodriguez Marie IsabelleRodriguez, Marie IsabelleÁlvarez Rodriguez, RosanaÁlvarez Rodriguez RosanaRodriguez de Lera ÁngelRodriguez de Lera, ÁngelGarcia-Rico Fernández, EduardoGarcia-Rico Fernández EduardoYu XiangYu, XiangCarregal Romero, SusanaCarregal Romero SusanaParak, Wolfgang JohannParak Wolfgang JohannVillanueva Leal CarlosVillanueva Leal, CarlosRivera Gil, PilarRivera Gil PilarÁlvarez Rodriguez SusanaÁlvarez Rodriguez, SusanaÁLVAREZ PUEBLA, Ramón ÁngelFENOLLOSA ESTEVE, RobertoMESSEGUER RICO, Francisco JavierRODRÍGUEZ, Marie IsabelleRodríguez Marie IsabelleÁlvarez Rodríguez SusanaÁLVAREZ RODRÍGUEZ, SusanaÁLVAREZ RODRÍGUEZ, RosanaÁlvarez Rodríguez RosanaRODRÍGUEZ de LERA, ÁngelRodríguez de Lera ÁngelGARCÍA-RICO FERNÁNDEZ, EduardoGarcía-Rico Fernández EduardoYU, XiangCARREGAL ROMERO, SusanaPARAK, Wolfgang JohannVILLANUEVA LEAL, CarlosRIVERA GIL, PilarRodríguez, Marie IsabelleÁlvarez Rodríguez, SusanaÁlvarez Rodríguez, RosanaRodríguez de Lera, ÁngelGarcía-Rico Fernández, Eduardo
Solicitantes
Universitat Rovira i VirgiliFundació Centre Tecnològic de la Química de CatalunyaInstitució Catalana de Recerca I Estudis Avançats IcreaInstitució Catalana de Recerca I Estudis AvançatsUniversitat Politècnica de ValènciaConsejo Superior de Investigaciones CientíficasUniversidade de VigoFundación Hospital de MadridPhilipps-Universität MarburgMedcomtech S.A.Phillips Univ Marburg
Clasificacion ipc
A61K 47/ 48 A IA61P 35/ 00 A IA61K 47/ 50 A IA61K 33/ 00 A IA61K 45/ 06 A IA61K 9/ 51 A IC07K 16/ 32 A I
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