RU2019125724A - Гиперстабилизированные липосомы, повышающие направленное таргетирование митотических клеток - Google Patents
Гиперстабилизированные липосомы, повышающие направленное таргетирование митотических клеток Download PDFInfo
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- RU2019125724A RU2019125724A RU2019125724A RU2019125724A RU2019125724A RU 2019125724 A RU2019125724 A RU 2019125724A RU 2019125724 A RU2019125724 A RU 2019125724A RU 2019125724 A RU2019125724 A RU 2019125724A RU 2019125724 A RU2019125724 A RU 2019125724A
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- Prior art keywords
- hyperstable
- hyperstable liposome
- acetate
- citrate
- phosphate
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- 239000002502 liposome Substances 0.000 title claims 19
- 230000000394 mitotic effect Effects 0.000 title 1
- 230000008685 targeting Effects 0.000 title 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 7
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 6
- 229910019142 PO4 Inorganic materials 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 6
- 239000010452 phosphate Substances 0.000 claims 6
- SXGZJKUKBWWHRA-UHFFFAOYSA-M 2-(N-morpholino)ethanesulfonate Chemical compound [O-]S(=O)(=O)CCN1CCOCC1 SXGZJKUKBWWHRA-UHFFFAOYSA-M 0.000 claims 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 150000001450 anions Chemical class 0.000 claims 4
- 230000002927 anti-mitotic effect Effects 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 239000012528 membrane Substances 0.000 claims 3
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 2
- QJZRFPJCWMNVAV-HHHXNRCGSA-N N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide Chemical compound NCCCN([C@H](C(C)C)C=1N(C(=O)C2=CC=C(Cl)C=C2N=1)CC=1C=CC=CC=1)C(=O)C1=CC=C(C)C=C1 QJZRFPJCWMNVAV-HHHXNRCGSA-N 0.000 claims 2
- XQVVPGYIWAGRNI-JOCHJYFZSA-N bi-2536 Chemical compound N1([C@@H](C(N(C)C2=CN=C(NC=3C(=CC(=CC=3)C(=O)NC3CCN(C)CC3)OC)N=C21)=O)CC)C1CCCC1 XQVVPGYIWAGRNI-JOCHJYFZSA-N 0.000 claims 2
- 150000001768 cations Chemical class 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- KGWWHPZQLVVAPT-STTJLUEPSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;6-(4-methylpiperazin-1-yl)-n-(5-methyl-1h-pyrazol-3-yl)-2-[(e)-2-phenylethenyl]pyrimidin-4-amine Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1CN(C)CCN1C1=CC(NC2=NNC(C)=C2)=NC(\C=C\C=2C=CC=CC=2)=N1 KGWWHPZQLVVAPT-STTJLUEPSA-N 0.000 claims 1
- MYBGWENAVMIGMM-GIFXNVAJSA-N (2s)-4-(2,5-difluorophenyl)-n-[(3r,4s)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-n-methyl-2-phenyl-2,5-dihydro-1h-pyrrole-1-carboxamide Chemical compound N1([C@](C=C(C1)C=1C(=CC=C(F)C=1)F)(CO)C=1C=CC=CC=1)C(=O)N(C)[C@H]1CCN(C)C[C@H]1F MYBGWENAVMIGMM-GIFXNVAJSA-N 0.000 claims 1
- FAYAUAZLLLJJGH-UHFFFAOYSA-N 1-(3-chlorophenyl)-3-[5-[2-(4-thieno[3,2-d]pyrimidinylamino)ethyl]-2-thiazolyl]urea Chemical compound ClC1=CC=CC(NC(=O)NC=2SC(CCNC=3C=4SC=CC=4N=CN=3)=CN=2)=C1 FAYAUAZLLLJJGH-UHFFFAOYSA-N 0.000 claims 1
- NHFDRBXTEDBWCZ-ZROIWOOFSA-N 3-[2,4-dimethyl-5-[(z)-(2-oxo-1h-indol-3-ylidene)methyl]-1h-pyrrol-3-yl]propanoic acid Chemical compound OC(=O)CCC1=C(C)NC(\C=C/2C3=CC=CC=C3NC\2=O)=C1C NHFDRBXTEDBWCZ-ZROIWOOFSA-N 0.000 claims 1
- HHFBDROWDBDFBR-UHFFFAOYSA-N 4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1NC1=NC=C(CN=C(C=2C3=CC=C(Cl)C=2)C=2C(=CC=CC=2F)F)C3=N1 HHFBDROWDBDFBR-UHFFFAOYSA-N 0.000 claims 1
- ZLHFILGSQDJULK-UHFFFAOYSA-N 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 ZLHFILGSQDJULK-UHFFFAOYSA-N 0.000 claims 1
- GPSZYOIFQZPWEJ-UHFFFAOYSA-N 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine Chemical compound N1=C(N)SC(C=2N=C(NC=3C=CC(=CC=3)N3CCOCC3)N=CC=2)=C1C GPSZYOIFQZPWEJ-UHFFFAOYSA-N 0.000 claims 1
- ZHJGWYRLJUCMRT-QGZVFWFLSA-N 5-[6-[(4-methyl-1-piperazinyl)methyl]-1-benzimidazolyl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide Chemical compound O([C@H](C)C=1C(=CC=CC=1)C(F)(F)F)C(=C(S1)C(N)=O)C=C1N(C1=C2)C=NC1=CC=C2CN1CCN(C)CC1 ZHJGWYRLJUCMRT-QGZVFWFLSA-N 0.000 claims 1
- GBJVVSCPOBPEIT-UHFFFAOYSA-N AZT-1152 Chemical compound N=1C=NC2=CC(OCCCN(CC)CCOP(O)(O)=O)=CC=C2C=1NC(=NN1)C=C1CC(=O)NC1=CC=CC(F)=C1 GBJVVSCPOBPEIT-UHFFFAOYSA-N 0.000 claims 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 1
- 229940123877 Aurora kinase inhibitor Drugs 0.000 claims 1
- -1 BI 811283 Chemical compound 0.000 claims 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 102000010638 Kinesin Human genes 0.000 claims 1
- 108010063296 Kinesin Proteins 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- XKFTZKGMDDZMJI-HSZRJFAPSA-N N-[5-[(2R)-2-methoxy-1-oxo-2-phenylethyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methyl-1-piperazinyl)benzamide Chemical compound O=C([C@H](OC)C=1C=CC=CC=1)N(CC=12)CC=1NN=C2NC(=O)C(C=C1)=CC=C1N1CCN(C)CC1 XKFTZKGMDDZMJI-HSZRJFAPSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims 1
- 239000003719 aurora kinase inhibitor Substances 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 229910052802 copper Inorganic materials 0.000 claims 1
- 239000010949 copper Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- LLXISKGBWFTGEI-FQEVSTJZSA-N filanesib Chemical compound C1([C@]2(CCCN)SC(=NN2C(=O)N(C)OC)C=2C(=CC=C(F)C=2)F)=CC=CC=C1 LLXISKGBWFTGEI-FQEVSTJZSA-N 0.000 claims 1
- 229950000133 filanesib Drugs 0.000 claims 1
- 229910052742 iron Inorganic materials 0.000 claims 1
- 229950007344 ispinesib Drugs 0.000 claims 1
- 239000011777 magnesium Substances 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- OBWNXGOQPLDDPS-UHFFFAOYSA-N n-(2,6-diethylphenyl)-3-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]-4,6-dihydro-1h-pyrrolo[3,4-c]pyrazole-5-carboxamide Chemical compound CCC1=CC=CC(CC)=C1NC(=O)N1CC(C(NC(=O)C=2C=CC(=CC=2)N2CCN(C)CC2)=NN2)=C2C1 OBWNXGOQPLDDPS-UHFFFAOYSA-N 0.000 claims 1
- PGXYIBJJCLWJST-MUUNZHRXSA-N n-(3-aminopropyl)-n-[(1r)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide Chemical compound NCCCN([C@H](C(C)C)C1=C(C(=O)C2=CC=C(Cl)C=C2O1)CC=1C=CC=CC=1)C(=O)C1=CC=C(C)C=C1 PGXYIBJJCLWJST-MUUNZHRXSA-N 0.000 claims 1
- OCKHRKSTDPOHEN-BQYQJAHWSA-N n-(4-methoxyphenyl)sulfonyl-n-[2-[(e)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)N(C(C)=O)C1=CC=CC=C1\C=C\C1=CC=[N+]([O-])C=C1 OCKHRKSTDPOHEN-BQYQJAHWSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000002770 polo like kinase inhibitor Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000012268 protein inhibitor Substances 0.000 claims 1
- 229940121649 protein inhibitor Drugs 0.000 claims 1
- OWBFCJROIKNMGD-BQYQJAHWSA-N rigosertib Chemical compound COC1=CC(OC)=CC(OC)=C1\C=C\S(=O)(=O)CC1=CC=C(OC)C(NCC(O)=O)=C1 OWBFCJROIKNMGD-BQYQJAHWSA-N 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- ZMANZCXQSJIPKH-UHFFFAOYSA-O triethylammonium ion Chemical compound CC[NH+](CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-O 0.000 claims 1
- SXNJFOWDRLKDSF-STROYTFGSA-N volasertib Chemical compound C1CN([C@H]2CC[C@@H](CC2)NC(=O)C2=CC=C(C(=C2)OC)NC=2N=C3N(C(C)C)[C@@H](C(N(C)C3=CN=2)=O)CC)CCN1CC1CC1 SXNJFOWDRLKDSF-STROYTFGSA-N 0.000 claims 1
- 239000011701 zinc Substances 0.000 claims 1
- 229910052725 zinc Inorganic materials 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
- A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
- A61K9/1277—Processes for preparing; Proliposomes
- A61K9/1278—Post-loading, e.g. by ion or pH gradient
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Dispersion Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Claims (17)
1. Гиперстабильная липосома, содержащая внутреннюю среду, отделенную от внешней среды мембраной, где внутренняя среда содержит противомитозное лекарственное средство, один или более анионов и один или более катионов, заключенных во внутреннюю среду, где заключенное противомитозное лекарственное средство выделяется с медленной скоростью, составляющей менее 0,6% за 12 часов или менее 5% за 8 дней, где липосомы суспендированы в 600 мМ сахарозе.
2. Гиперстабильная липосома по п. 1, где одним или более анионами являются цитрат, ацетат, фосфат, 2-(N-морфолино)этансульфонат, хлорид, цитрат и ацетат, цитрат и 2-(N-морфолино)этансульфонат, цитрат и хлорид, ацетат и фосфат, ацетат и 2-(N-морфолино)этансульфонат, ацетат и хлорид, фосфат и 2-(N-морфолино)этансульфонат, фосфат и хлорид, 2-(N-морфолино)этансульфонат и хлорид.
3. Гиперстабильная липосома по п. 1 или 2, где два аниона представлены в соотношении от около 1:7 до около 7:1.
4. Гиперстабильная липосома по п. 3, где одним или более анионами являются цитрат и фосфат или цитрат и ацетат или ацетат и фосфат.
5. Гиперстабильная липосома по любому из пп. 1-4, где одним или боле катионов являются натрий, аммоний, триэтиламмоний, медь, магний, цинк или железо.
6. Гиперстабильная липосома по любому из пп. 1-5, где противомитозным лекарственным средством является ингибиторы polo-подобных киназ, такие как BI2536, ON01910, GSK 461364, HMN 214 или BI 6727; ингибитор кинезин-веретенообразного белка, такой как Испинесиб (SB 715992), SB 743921, MK 0731 или ARRY 520; или ингибитор аврора-киназы, такой как MK 0457 (VX 680), AZD 1152, PHA 680632, PHA 739358, MLN8054, MLN8237, R763, AT9283, SNS 314, SU 6668, ENMD 2076, BI 811283, CYC116, ENMD 981693 или MKC 1693.
7. Гиперстабильная липосома по п. 6, где противомитозным лекарственным средством является BI 2536 или Испинесиб.
8. Гиперстабильная липосома по любому из пп. 1-7, где мембрана содержит 1,2-дистеароил-sn-глицерин-3-фосфоэтаноламин-N-[метокси(полиэтиленгликоль)-2000] (ДСФЭ-ПЭГ2000), гидрированный яичный L-α-фосфатидилхолин (ГЯФХ) и холестерин (Хол).
9. Гиперстабильная липосома по п. 8, где мембрана содержит ГЯФХ:Хол:ДСФЭ-ПЭГ2000 в молярном соотношении 50:45:5.
10. Липосомальная композиция, содержащая гиперстабильную липосому по любому из пп. 1-9 в водной среде.
11. Фармацевтическая композиция, содержащая гиперстабильную липосому по любому из пп 1-9.
12. Фармацевтическая композиция по п. 11, где композиция дополнительно содержит по меньшей мере один фармацевтически приемлемый эксципиент и/или носитель.
13. Способ лечения рака у субъекта, включающий введение терапевтически эффективного количества гиперстабильной липосомы по любому из пп. 1-9 или липосомальной композиции по п. 10 или фармацевтической композиции по п. 11 или 12 нуждающемуся в этом субъекту.
14. Применение гиперстабильной липосомы по любому из пп. 1-9 в приготовлении лекарственного средства для лечения рака у субъекта.
15. Применение гиперстабильной липосомы по любому из пп. 1-9 или липосомальной композиции по п. 10 или фармацевтической композиции по п. 11 или 12 для лечения рака у субъекта.
16. Гиперстабильная липосома по любому из пп. 1-9 для применения в приготовлении лекарственного средства для лечения рака у субъекта.
17. Гиперстабильная липосома по любому из пп. 1-9, или липосомальной композиции по п. 10, или фармацевтической композиции по п. 11 или 12 для применения в лечении рака у субъекта.
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| AU2002334358B2 (en) | 2001-09-06 | 2008-02-07 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | A method for preparing liposome formulations with a predefined release profile |
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| NZ711500A (en) * | 2013-03-15 | 2020-05-29 | Taiwan Liposome Co Ltd | Engineering a control drug release profile via liposome compositions in both aqueous and non-aqueous compartments |
| CN106659683A (zh) * | 2014-01-14 | 2017-05-10 | 约翰斯·霍普金斯大学 | 包封修饰的环糊精复合物的脂质体组合物及其应用 |
| US20170035894A1 (en) * | 2014-04-14 | 2017-02-09 | Endocyte, Inc. | Drug delivery conjugates for treating resistant cancer and for use in combination therapy |
| US20160175250A1 (en) * | 2014-12-23 | 2016-06-23 | Tolmar Inc. | Method for Making Liposomes Containing an Active Pharmaceutical Ingredient |
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