DK2750683T3 - Nanopartikler, fremgangsmåder til fremstilling og anvendelse deraf som bærer for amfipatiske eller hydrofobe molekyler i området af medicin indbefattende cancerbehandling og fødevareforbundne forbindelser - Google Patents

Nanopartikler, fremgangsmåder til fremstilling og anvendelse deraf som bærer for amfipatiske eller hydrofobe molekyler i området af medicin indbefattende cancerbehandling og fødevareforbundne forbindelser Download PDF

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DK2750683T3
DK2750683T3 DK12781489.5T DK12781489T DK2750683T3 DK 2750683 T3 DK2750683 T3 DK 2750683T3 DK 12781489 T DK12781489 T DK 12781489T DK 2750683 T3 DK2750683 T3 DK 2750683T3
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nanoparticles
quillaja
saponin
cholesterol
cells
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DK2750683T4 (da
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Bror Morein
Saideh Berenjian
Kefei Hu
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Mx Adjuvac Ab
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    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
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    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
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    • A61K2039/55577—Saponins; Quil A; QS21; ISCOMS
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Claims (14)

1. Stabile nanopartikler omfattende sterol, fortrinsvis kolesterol og en bestanddel fra Quillaja saponaria Molina valgt blandt quillajasyre og quillaja-saponin, kendetegnet ved at nanopartiklerne ikke omfatter et fosforlipid, har en partikeldiameter i intervallet 15-25 nanometer, og hvor forholdet mellem kolesterol og quillaja-saponin er fra 1:10 til 10:1, fortrinsvis fra 1:2 til 2:1.
2. Nanopartikler ifølge krav 1, hvor quillajabestanddelen er et quillaja-saponin, fortrinsvis quillaja-saponin-fraktion QHA, QHB og/eller QHC.
3. Nanopartikler ifølge krav 1 omfattende kolesterol og quillaja-saponin-fraktionen QHC, hvor partiklerne har en diameter på omkring 17-20 nm, og hvor det molære forhold mellem kolesterol og QHC er omkring 1:1.
4. Nanopartikler ifølge et hvilket som helst af de forgående krav yderligere omfattende mindst ét amfipatisk eller et hydrofobt molekyle.
5. Nanopartikler ifølge krav 3 eller 4, hvor de amfipatiske eller hydrofobe molekyler er mindst ét element valgt blandt et antigen, et adjuvans, et målsøgende molekyle (ENG: a targeting molecule), en farmaceutisk forbindelse eller en fødevareforbundet forbindelse.
6. Nanopartikler ifølge krav 5, hvor det amfipatiske eller hydrofobe molekyle er mindst ét element valgt blandt diterpen DT, VLX40, Busulfan, roscovitin og vitamin D3.
7. Sammensætning omfattende én eller flere nanopartikler ifølge et hvilket som helst af krav 1-6.
8. Sammensætning ifølge krav 7, hvor forskellige quillaja-saponinfraktioner hver især er inkorporeret i forskellige nanopartikler.
9. Nanopartikel ifølge et hvilket som helst af krav 1-6 eller en sammensætning ifølge et hvilket som helst af krav 7 eller 8 til anvendelse som et lægemiddel eventuelt i en farmaceutisk sammensætning yderligere omfattende farmaceutisk acceptable puffere, fortyndingsmidler, excipienser, adjuvanser, og/eller bærere.
10. Nanopartikel ifølge et hvilket som helst af krav 1-6 eller en sammensætning ifølge et hvilket som helst af krav 7 og 8 til anvendelse som et adjuvans.
11. Farmaceutisk adjuvans ifølge krav 10 til anvendelse i kombination med en vaccine.
12. Nanopartikel ifølge et hvilket som helst af krav 1-6 eller en sammensætning ifølge et hvilket som helst af krav 7 og 8 til anvendelse som et anti-cancermiddel.
13. Fremgangsmåde til fremstilling af fosforlipid-frie nanopartikler omfattende trinnene, at a) frembringe en hydrofob overflade b) bringe den hydrofobe overflade i kontakt med en opløsning af sterol, fortrinsvis kolesterol opløst som monomerer i et organisk opløsningsmiddel eller detergent; c) fjerne opløsningsmidlet eller detergenten under dannelse af en sterolmembran på overfladen d) frembringe en vandopløsning af quillaja-saponin-miceller e) tilsætte vandopløsningen omfattende saponinmicellerne til sterolmembranen, hvorved et kompleks dannes mellem saponinerne og sterolerne og suspenderes i vandopløsningen, og hvor forholdet mellem kolesterol og quillaja-saponin er fra 1:10 til 10:1, fortrinsvis fra 1:2 til 2:1.
14. Fremgangsmåde til vurdering af anvendeligheden af et anti-cancermiddel ifølge krav 12, omfattende at a) bringe cancercellerne fra en patient i kontakt in vitro med nanopartikler ifølge et hvilket som helst af krav 1-6 eller en farmaceutisk sammensætning ifølge krav 7 eller 8; b) måle mindst én virkning indikativ for terapeutisk virkning af nanopartiklerne eller den farmaceutiske sammensætning på cancercellerne; hvor anti-cancermidlet vurderes som anvendelig for den enkelte patient, hvis nanopartiklerne eller den farmaceutiske sammensætning viser en signifikant virkning på cancercellerne.
DK12781489.5T 2011-10-03 2012-10-01 Nanopartikler, fremgangsmåde til fremstilling og anvendelse deraf som bærer for amfipatiske eller hydrofobe molekyler inden for medicin, herunder cancerbehandling, og i fødevarerelaterede forbindelser DK2750683T4 (da)

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PCT/SE2012/051048 WO2013051994A1 (en) 2011-10-03 2012-10-01 Nanoparticles, process for preparation and use thereof as carrier for amphipatic of hydrophobic molecules in fields of medicine including cancer treatment and food related compounds

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