JP5947807B2 - ナノ粒子組成物への放射性核種の封入 - Google Patents
ナノ粒子組成物への放射性核種の封入 Download PDFInfo
- Publication number
- JP5947807B2 JP5947807B2 JP2013543530A JP2013543530A JP5947807B2 JP 5947807 B2 JP5947807 B2 JP 5947807B2 JP 2013543530 A JP2013543530 A JP 2013543530A JP 2013543530 A JP2013543530 A JP 2013543530A JP 5947807 B2 JP5947807 B2 JP 5947807B2
- Authority
- JP
- Japan
- Prior art keywords
- iii
- nanoparticles
- metal body
- encapsulation
- liposome
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 239000002105 nanoparticle Substances 0.000 title claims description 252
- 238000005538 encapsulation Methods 0.000 title claims description 215
- 239000000203 mixture Substances 0.000 title claims description 159
- 239000010949 copper Substances 0.000 claims description 386
- 229910052751 metal Inorganic materials 0.000 claims description 159
- 239000002184 metal Substances 0.000 claims description 159
- 238000000034 method Methods 0.000 claims description 142
- 150000001768 cations Chemical class 0.000 claims description 121
- 239000012528 membrane Substances 0.000 claims description 105
- 239000002738 chelating agent Substances 0.000 claims description 96
- 239000002555 ionophore Substances 0.000 claims description 90
- 230000000236 ionophoric effect Effects 0.000 claims description 89
- 229910052802 copper Inorganic materials 0.000 claims description 64
- 150000002632 lipids Chemical class 0.000 claims description 59
- 229910052733 gallium Inorganic materials 0.000 claims description 56
- NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims description 50
- 150000002500 ions Chemical class 0.000 claims description 48
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 45
- 229910052688 Gadolinium Inorganic materials 0.000 claims description 37
- 229910052765 Lutetium Inorganic materials 0.000 claims description 36
- 230000003204 osmotic effect Effects 0.000 claims description 35
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims description 34
- 238000004519 manufacturing process Methods 0.000 claims description 34
- 229910052742 iron Inorganic materials 0.000 claims description 31
- 150000001875 compounds Chemical class 0.000 claims description 28
- 230000005855 radiation Effects 0.000 claims description 26
- 229910052692 Dysprosium Inorganic materials 0.000 claims description 25
- 230000003647 oxidation Effects 0.000 claims description 25
- 238000007254 oxidation reaction Methods 0.000 claims description 25
- 229910052713 technetium Inorganic materials 0.000 claims description 24
- 229910052716 thallium Inorganic materials 0.000 claims description 24
- 229910052804 chromium Inorganic materials 0.000 claims description 23
- 229910052748 manganese Inorganic materials 0.000 claims description 23
- 229910052759 nickel Inorganic materials 0.000 claims description 22
- VTLYFUHAOXGGBS-UHFFFAOYSA-N Fe3+ Chemical compound [Fe+3] VTLYFUHAOXGGBS-UHFFFAOYSA-N 0.000 claims description 20
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims description 19
- 239000010931 gold Substances 0.000 claims description 19
- 229910052727 yttrium Inorganic materials 0.000 claims description 18
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims description 14
- FZLIPJUXYLNCLC-UHFFFAOYSA-N lanthanum atom Chemical compound [La] FZLIPJUXYLNCLC-UHFFFAOYSA-N 0.000 claims description 12
- YACKEPLHDIMKIO-UHFFFAOYSA-N methylphosphonic acid Chemical compound CP(O)(O)=O YACKEPLHDIMKIO-UHFFFAOYSA-N 0.000 claims description 12
- 150000003904 phospholipids Chemical class 0.000 claims description 11
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims description 9
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims description 9
- 238000012258 culturing Methods 0.000 claims description 9
- 229960003330 pentetic acid Drugs 0.000 claims description 9
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 8
- KILNVBDSWZSGLL-KXQOOQHDSA-N 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCC KILNVBDSWZSGLL-KXQOOQHDSA-N 0.000 claims description 7
- MDAXKAUIABOHTD-UHFFFAOYSA-N 1,4,8,11-tetraazacyclotetradecane Chemical compound C1CNCCNCCCNCCNC1 MDAXKAUIABOHTD-UHFFFAOYSA-N 0.000 claims description 7
- GYHNNYVSQQEPJS-UHFFFAOYSA-N Gallium Chemical compound [Ga] GYHNNYVSQQEPJS-UHFFFAOYSA-N 0.000 claims description 7
- VWQVUPCCIRVNHF-OUBTZVSYSA-N Yttrium-90 Chemical compound [90Y] VWQVUPCCIRVNHF-OUBTZVSYSA-N 0.000 claims description 7
- 229910052767 actinium Inorganic materials 0.000 claims description 7
- QQINRWTZWGJFDB-UHFFFAOYSA-N actinium atom Chemical compound [Ac] QQINRWTZWGJFDB-UHFFFAOYSA-N 0.000 claims description 7
- 229910052787 antimony Inorganic materials 0.000 claims description 7
- WATWJIUSRGPENY-UHFFFAOYSA-N antimony atom Chemical compound [Sb] WATWJIUSRGPENY-UHFFFAOYSA-N 0.000 claims description 7
- RYXHOMYVWAEKHL-UHFFFAOYSA-N astatine atom Chemical compound [At] RYXHOMYVWAEKHL-UHFFFAOYSA-N 0.000 claims description 7
- 125000002091 cationic group Chemical group 0.000 claims description 7
- OHSVLFRHMCKCQY-UHFFFAOYSA-N lutetium atom Chemical compound [Lu] OHSVLFRHMCKCQY-UHFFFAOYSA-N 0.000 claims description 7
- 229910052702 rhenium Inorganic materials 0.000 claims description 7
- WUAPFZMCVAUBPE-UHFFFAOYSA-N rhenium atom Chemical compound [Re] WUAPFZMCVAUBPE-UHFFFAOYSA-N 0.000 claims description 7
- BKVIYDNLLOSFOA-UHFFFAOYSA-N thallium Chemical compound [Tl] BKVIYDNLLOSFOA-UHFFFAOYSA-N 0.000 claims description 7
- QBPPRVHXOZRESW-UHFFFAOYSA-N 1,4,7,10-tetraazacyclododecane Chemical group C1CNCCNCCNCCN1 QBPPRVHXOZRESW-UHFFFAOYSA-N 0.000 claims description 6
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims description 6
- 229910052772 Samarium Inorganic materials 0.000 claims description 6
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims description 6
- 229910052789 astatine Inorganic materials 0.000 claims description 6
- 229910052788 barium Inorganic materials 0.000 claims description 6
- DSAJWYNOEDNPEQ-UHFFFAOYSA-N barium atom Chemical compound [Ba] DSAJWYNOEDNPEQ-UHFFFAOYSA-N 0.000 claims description 6
- 229910052793 cadmium Inorganic materials 0.000 claims description 6
- BDOSMKKIYDKNTQ-UHFFFAOYSA-N cadmium atom Chemical compound [Cd] BDOSMKKIYDKNTQ-UHFFFAOYSA-N 0.000 claims description 6
- 229910017052 cobalt Inorganic materials 0.000 claims description 6
- 239000010941 cobalt Substances 0.000 claims description 6
- GUTLYIVDDKVIGB-UHFFFAOYSA-N cobalt atom Chemical compound [Co] GUTLYIVDDKVIGB-UHFFFAOYSA-N 0.000 claims description 6
- BJAJDJDODCWPNS-UHFFFAOYSA-N dotp Chemical compound O=C1N2CCOC2=NC2=C1SC=C2 BJAJDJDODCWPNS-UHFFFAOYSA-N 0.000 claims description 6
- KBQHZAAAGSGFKK-UHFFFAOYSA-N dysprosium atom Chemical compound [Dy] KBQHZAAAGSGFKK-UHFFFAOYSA-N 0.000 claims description 6
- UIWYJDYFSGRHKR-UHFFFAOYSA-N gadolinium atom Chemical compound [Gd] UIWYJDYFSGRHKR-UHFFFAOYSA-N 0.000 claims description 6
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 claims description 6
- 229910052737 gold Inorganic materials 0.000 claims description 6
- 229910052746 lanthanum Inorganic materials 0.000 claims description 6
- 229910052763 palladium Inorganic materials 0.000 claims description 6
- 229910052705 radium Inorganic materials 0.000 claims description 6
- HCWPIIXVSYCSAN-UHFFFAOYSA-N radium atom Chemical compound [Ra] HCWPIIXVSYCSAN-UHFFFAOYSA-N 0.000 claims description 6
- 229910052707 ruthenium Inorganic materials 0.000 claims description 6
- KZUNJOHGWZRPMI-UHFFFAOYSA-N samarium atom Chemical compound [Sm] KZUNJOHGWZRPMI-UHFFFAOYSA-N 0.000 claims description 6
- 229910052712 strontium Inorganic materials 0.000 claims description 6
- CIOAGBVUUVVLOB-UHFFFAOYSA-N strontium atom Chemical compound [Sr] CIOAGBVUUVVLOB-UHFFFAOYSA-N 0.000 claims description 6
- GKLVYJBZJHMRIY-UHFFFAOYSA-N technetium atom Chemical compound [Tc] GKLVYJBZJHMRIY-UHFFFAOYSA-N 0.000 claims description 6
- 229910052714 tellurium Inorganic materials 0.000 claims description 6
- PORWMNRCUJJQNO-UHFFFAOYSA-N tellurium atom Chemical compound [Te] PORWMNRCUJJQNO-UHFFFAOYSA-N 0.000 claims description 6
- NAWDYIZEMPQZHO-AHCXROLUSA-N ytterbium-169 Chemical compound [169Yb] NAWDYIZEMPQZHO-AHCXROLUSA-N 0.000 claims description 6
- YDVODBIDDSGKAD-UHFFFAOYSA-N 1,4,7,11-tetrazacyclotetradecane Chemical compound C1CNCCCNCCNCCNC1 YDVODBIDDSGKAD-UHFFFAOYSA-N 0.000 claims description 5
- 229910052771 Terbium Inorganic materials 0.000 claims description 5
- GZCRRIHWUXGPOV-UHFFFAOYSA-N terbium atom Chemical compound [Tb] GZCRRIHWUXGPOV-UHFFFAOYSA-N 0.000 claims description 5
- 229940106189 ceramide Drugs 0.000 claims description 4
- 238000011534 incubation Methods 0.000 claims description 4
- LADZJJOUGVGJHM-UHFFFAOYSA-N 1,4,7,10-tetrazacyclotridecane Chemical compound C1CNCCNCCNCCNC1 LADZJJOUGVGJHM-UHFFFAOYSA-N 0.000 claims description 3
- TWMXRTUIOCTFNL-UHFFFAOYSA-N 1,5,8,12-tetrazabicyclo[10.2.2]hexadecane Chemical group C1CN2CCN1CCCNCCNCCC2 TWMXRTUIOCTFNL-UHFFFAOYSA-N 0.000 claims description 3
- HHLZCENAOIROSL-UHFFFAOYSA-N 2-[4,7-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid Chemical compound OC(=O)CN1CCNCCN(CC(O)=O)CCN(CC(O)=O)CC1 HHLZCENAOIROSL-UHFFFAOYSA-N 0.000 claims description 3
- SPSJFVXUOKRIGT-UHFFFAOYSA-N 2-[7-(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid Chemical compound OC(=O)CN1CCNCCN(CC(O)=O)CCNCC1 SPSJFVXUOKRIGT-UHFFFAOYSA-N 0.000 claims description 3
- 229910052738 indium Inorganic materials 0.000 claims description 3
- APFVFJFRJDLVQX-UHFFFAOYSA-N indium atom Chemical compound [In] APFVFJFRJDLVQX-UHFFFAOYSA-N 0.000 claims description 3
- 150000003408 sphingolipids Chemical class 0.000 claims description 3
- YXPRJLINFVQPDT-UHFFFAOYSA-N 1,5,9,13-tetrazacyclohexadecane Chemical compound C1CNCCCNCCCNCCCNC1 YXPRJLINFVQPDT-UHFFFAOYSA-N 0.000 claims description 2
- XDLOGHYCUQYEKA-UHFFFAOYSA-N 2-(1,4,7,10-tetrazacyclododec-1-yl)acetic acid Chemical compound OC(=O)CN1CCNCCNCCNCC1 XDLOGHYCUQYEKA-UHFFFAOYSA-N 0.000 claims description 2
- HDKPQQZMQBYEHX-UHFFFAOYSA-N 2-(4,8,11-triaza-1-azoniacyclotetradec-1-yl)acetate Chemical compound OC(=O)CN1CCCNCCNCCCNCC1 HDKPQQZMQBYEHX-UHFFFAOYSA-N 0.000 claims description 2
- 150000001783 ceramides Chemical class 0.000 claims description 2
- KUFDRRWNPNXBRF-UHFFFAOYSA-N 1,4,8,12-tetrazacyclopentadecane Chemical compound C1CNCCCNCCNCCCNC1 KUFDRRWNPNXBRF-UHFFFAOYSA-N 0.000 claims 1
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 claims 1
- 101001105486 Homo sapiens Proteasome subunit alpha type-7 Proteins 0.000 claims 1
- 102100021201 Proteasome subunit alpha type-7 Human genes 0.000 claims 1
- WDJHALXBUFZDSR-UHFFFAOYSA-N acetoacetic acid Chemical compound CC(=O)CC(O)=O WDJHALXBUFZDSR-UHFFFAOYSA-N 0.000 claims 1
- 101150040681 cho1 gene Proteins 0.000 claims 1
- 239000002502 liposome Substances 0.000 description 278
- 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 description 104
- 229920001223 polyethylene glycol Polymers 0.000 description 57
- 239000000126 substance Substances 0.000 description 56
- 235000012000 cholesterol Nutrition 0.000 description 52
- 206010028980 Neoplasm Diseases 0.000 description 40
- 238000001542 size-exclusion chromatography Methods 0.000 description 37
- 201000011510 cancer Diseases 0.000 description 33
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 29
- 239000002202 Polyethylene glycol Substances 0.000 description 29
- 230000000694 effects Effects 0.000 description 29
- APFVFJFRJDLVQX-AHCXROLUSA-N indium-111 Chemical compound [111In] APFVFJFRJDLVQX-AHCXROLUSA-N 0.000 description 29
- 229910021645 metal ion Inorganic materials 0.000 description 29
- 239000007995 HEPES buffer Substances 0.000 description 28
- 239000000243 solution Substances 0.000 description 27
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 24
- -1 pH gradients Substances 0.000 description 23
- 235000021588 free fatty acids Nutrition 0.000 description 22
- 230000002285 radioactive effect Effects 0.000 description 22
- 238000004809 thin layer chromatography Methods 0.000 description 19
- 239000003814 drug Substances 0.000 description 18
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 18
- 239000000872 buffer Substances 0.000 description 17
- 238000012544 monitoring process Methods 0.000 description 17
- 201000010099 disease Diseases 0.000 description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 16
- 229940079593 drug Drugs 0.000 description 16
- 238000003384 imaging method Methods 0.000 description 16
- 238000011282 treatment Methods 0.000 description 16
- 230000006870 function Effects 0.000 description 15
- 229910052757 nitrogen Inorganic materials 0.000 description 15
- 210000001519 tissue Anatomy 0.000 description 15
- 208000032843 Hemorrhage Diseases 0.000 description 14
- 230000000740 bleeding effect Effects 0.000 description 14
- 239000000463 material Substances 0.000 description 14
- 238000003325 tomography Methods 0.000 description 14
- 210000004204 blood vessel Anatomy 0.000 description 13
- 235000014113 dietary fatty acids Nutrition 0.000 description 13
- 238000009792 diffusion process Methods 0.000 description 13
- 229930195729 fatty acid Natural products 0.000 description 13
- 239000000194 fatty acid Substances 0.000 description 13
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 12
- 239000011780 sodium chloride Substances 0.000 description 12
- 230000008859 change Effects 0.000 description 11
- 238000002474 experimental method Methods 0.000 description 11
- 239000012071 phase Substances 0.000 description 11
- 238000002360 preparation method Methods 0.000 description 11
- 230000032258 transport Effects 0.000 description 11
- 238000002354 inductively-coupled plasma atomic emission spectroscopy Methods 0.000 description 10
- 230000008723 osmotic stress Effects 0.000 description 10
- 239000002245 particle Substances 0.000 description 10
- 230000035699 permeability Effects 0.000 description 10
- 238000001959 radiotherapy Methods 0.000 description 10
- 108091006671 Ion Transporter Proteins 0.000 description 9
- 102000037862 Ion Transporter Human genes 0.000 description 9
- 239000008346 aqueous phase Substances 0.000 description 9
- 150000004665 fatty acids Chemical class 0.000 description 9
- 229920000642 polymer Polymers 0.000 description 9
- 108090000765 processed proteins & peptides Proteins 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- 238000002603 single-photon emission computed tomography Methods 0.000 description 9
- 230000001225 therapeutic effect Effects 0.000 description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 8
- 229920005654 Sephadex Polymers 0.000 description 8
- 239000012507 Sephadex™ Substances 0.000 description 8
- 239000007864 aqueous solution Substances 0.000 description 8
- 238000003745 diagnosis Methods 0.000 description 8
- 230000002209 hydrophobic effect Effects 0.000 description 8
- MCJGNVYPOGVAJF-UHFFFAOYSA-N quinolin-8-ol Chemical compound C1=CN=C2C(O)=CC=CC2=C1 MCJGNVYPOGVAJF-UHFFFAOYSA-N 0.000 description 8
- 239000011734 sodium Substances 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 8
- 230000008685 targeting Effects 0.000 description 8
- 230000001276 controlling effect Effects 0.000 description 7
- 238000000502 dialysis Methods 0.000 description 7
- 238000004255 ion exchange chromatography Methods 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 229910021591 Copper(I) chloride Inorganic materials 0.000 description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- 239000000232 Lipid Bilayer Substances 0.000 description 6
- 210000004027 cell Anatomy 0.000 description 6
- 238000006243 chemical reaction Methods 0.000 description 6
- OXBLHERUFWYNTN-UHFFFAOYSA-M copper(I) chloride Chemical compound [Cu]Cl OXBLHERUFWYNTN-UHFFFAOYSA-M 0.000 description 6
- 238000010828 elution Methods 0.000 description 6
- 238000001095 inductively coupled plasma mass spectrometry Methods 0.000 description 6
- 238000002595 magnetic resonance imaging Methods 0.000 description 6
- 230000001575 pathological effect Effects 0.000 description 6
- 102000004169 proteins and genes Human genes 0.000 description 6
- 108090000623 proteins and genes Proteins 0.000 description 6
- 239000012217 radiopharmaceutical Substances 0.000 description 6
- 229940121896 radiopharmaceutical Drugs 0.000 description 6
- 230000002799 radiopharmaceutical effect Effects 0.000 description 6
- DPEGQJDYRIQRHI-UHFFFAOYSA-N 8-Chinolinyl-6-A Natural products O1C(C(O)=O)C(O)C(O)C(O)C1OC1=CC=CC2=CC=CN=C12 DPEGQJDYRIQRHI-UHFFFAOYSA-N 0.000 description 5
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 5
- JVHROZDXPAUZFK-UHFFFAOYSA-N TETA Chemical compound OC(=O)CN1CCCN(CC(O)=O)CCN(CC(O)=O)CCCN(CC(O)=O)CC1 JVHROZDXPAUZFK-UHFFFAOYSA-N 0.000 description 5
- 239000003638 chemical reducing agent Substances 0.000 description 5
- 230000007423 decrease Effects 0.000 description 5
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 5
- 238000001727 in vivo Methods 0.000 description 5
- 230000014759 maintenance of location Effects 0.000 description 5
- 230000007935 neutral effect Effects 0.000 description 5
- 229960003540 oxyquinoline Drugs 0.000 description 5
- 239000012466 permeate Substances 0.000 description 5
- 239000002953 phosphate buffered saline Substances 0.000 description 5
- 230000008569 process Effects 0.000 description 5
- 102000004196 processed proteins & peptides Human genes 0.000 description 5
- 235000018102 proteins Nutrition 0.000 description 5
- 238000000746 purification Methods 0.000 description 5
- 210000002966 serum Anatomy 0.000 description 5
- 238000003860 storage Methods 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 239000005725 8-Hydroxyquinoline Substances 0.000 description 4
- 229930182558 Sterol Natural products 0.000 description 4
- MWTIGLPPQBNUFP-RRHRGVEJSA-N [(2r)-2,3-dihexadecoxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical compound CCCCCCCCCCCCCCCCOC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OCCCCCCCCCCCCCCCC MWTIGLPPQBNUFP-RRHRGVEJSA-N 0.000 description 4
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical class C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 description 4
- 210000004556 brain Anatomy 0.000 description 4
- 239000000969 carrier Substances 0.000 description 4
- BQYIXOPJPLGCRZ-REZTVBANSA-N chembl103111 Chemical compound CC1=NC=C(CO)C(\C=N\NC(=O)C=2C=CN=CC=2)=C1O BQYIXOPJPLGCRZ-REZTVBANSA-N 0.000 description 4
- 230000004087 circulation Effects 0.000 description 4
- 238000007796 conventional method Methods 0.000 description 4
- 238000001514 detection method Methods 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 230000033001 locomotion Effects 0.000 description 4
- 230000003211 malignant effect Effects 0.000 description 4
- RJIWZDNTCBHXAL-UHFFFAOYSA-N nitroxoline Chemical compound C1=CN=C2C(O)=CC=C([N+]([O-])=O)C2=C1 RJIWZDNTCBHXAL-UHFFFAOYSA-N 0.000 description 4
- 210000000056 organ Anatomy 0.000 description 4
- 239000003960 organic solvent Substances 0.000 description 4
- 239000004417 polycarbonate Substances 0.000 description 4
- 229920000515 polycarbonate Polymers 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 238000000926 separation method Methods 0.000 description 4
- 150000003432 sterols Chemical class 0.000 description 4
- 235000003702 sterols Nutrition 0.000 description 4
- 125000002730 succinyl group Chemical group C(CCC(=O)*)(=O)* 0.000 description 4
- 230000007704 transition Effects 0.000 description 4
- BWMXDESAZVPVGR-BGNCJLHMSA-N (2r,3r,4s,5r,6s)-2-(hydroxymethyl)-6-quinolin-8-yloxyoxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1OC1=CC=CC2=CC=CN=C12 BWMXDESAZVPVGR-BGNCJLHMSA-N 0.000 description 3
- BWMXDESAZVPVGR-TVKJYDDYSA-N (2r,3s,4s,5r,6s)-2-(hydroxymethyl)-6-quinolin-8-yloxyoxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=CC2=CC=CN=C12 BWMXDESAZVPVGR-TVKJYDDYSA-N 0.000 description 3
- DPEGQJDYRIQRHI-DKBOKBLXSA-N (2s,3s,4s,5r,6s)-3,4,5-trihydroxy-6-quinolin-8-yloxyoxane-2-carboxylic acid Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC1=CC=CC2=CC=CN=C12 DPEGQJDYRIQRHI-DKBOKBLXSA-N 0.000 description 3
- VTQDJAUGGZFPOI-UHFFFAOYSA-N (8-hydroxyquinolin-1-ium-5-yl)azanium;dichloride Chemical compound Cl.Cl.C1=CC=C2C(N)=CC=C(O)C2=N1 VTQDJAUGGZFPOI-UHFFFAOYSA-N 0.000 description 3
- AWKZSNHJRJMXCN-UHFFFAOYSA-N 2-[butyl-(8-hydroxyquinolin-2-yl)amino]quinolin-8-ol Chemical compound C1=CC=C(O)C2=NC(N(C=3N=C4C(O)=CC=CC4=CC=3)CCCC)=CC=C21 AWKZSNHJRJMXCN-UHFFFAOYSA-N 0.000 description 3
- ADJQQSUBKRASQN-UHFFFAOYSA-N 7-bromo-5-chloroquinolin-8-ol Chemical compound C1=CN=C2C(O)=C(Br)C=C(Cl)C2=C1 ADJQQSUBKRASQN-UHFFFAOYSA-N 0.000 description 3
- FJKUOCCQEBLPNX-UHFFFAOYSA-N 8-hydroxyquinoline N-oxide Chemical compound C1=C[N+]([O-])=C2C(O)=CC=CC2=C1 FJKUOCCQEBLPNX-UHFFFAOYSA-N 0.000 description 3
- LGDFHDKSYGVKDC-UHFFFAOYSA-N 8-hydroxyquinoline-5-sulfonic acid Chemical compound C1=CN=C2C(O)=CC=C(S(O)(=O)=O)C2=C1 LGDFHDKSYGVKDC-UHFFFAOYSA-N 0.000 description 3
- 208000009458 Carcinoma in Situ Diseases 0.000 description 3
- 229930186217 Glycolipid Natural products 0.000 description 3
- 241000124008 Mammalia Species 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 229940111121 antirheumatic drug quinolines Drugs 0.000 description 3
- 210000001188 articular cartilage Anatomy 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 239000003012 bilayer membrane Substances 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 210000000988 bone and bone Anatomy 0.000 description 3
- 239000007853 buffer solution Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- WDFKMLRRRCGAKS-UHFFFAOYSA-N chloroxine Chemical compound C1=CN=C2C(O)=C(Cl)C=C(Cl)C2=C1 WDFKMLRRRCGAKS-UHFFFAOYSA-N 0.000 description 3
- GPTXWRGISTZRIO-UHFFFAOYSA-N chlorquinaldol Chemical compound ClC1=CC(Cl)=C(O)C2=NC(C)=CC=C21 GPTXWRGISTZRIO-UHFFFAOYSA-N 0.000 description 3
- 239000008393 encapsulating agent Substances 0.000 description 3
- 210000001508 eye Anatomy 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 210000004392 genitalia Anatomy 0.000 description 3
- 201000004933 in situ carcinoma Diseases 0.000 description 3
- 230000002757 inflammatory effect Effects 0.000 description 3
- UXZFQZANDVDGMM-UHFFFAOYSA-N iodoquinol Chemical compound C1=CN=C2C(O)=C(I)C=C(I)C2=C1 UXZFQZANDVDGMM-UHFFFAOYSA-N 0.000 description 3
- 210000000244 kidney pelvis Anatomy 0.000 description 3
- 239000003446 ligand Substances 0.000 description 3
- 239000007791 liquid phase Substances 0.000 description 3
- 150000003248 quinolines Chemical class 0.000 description 3
- 238000009790 rate-determining step (RDS) Methods 0.000 description 3
- 238000007789 sealing Methods 0.000 description 3
- 210000004872 soft tissue Anatomy 0.000 description 3
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 description 3
- 241000894007 species Species 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 150000008163 sugars Chemical class 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 238000010998 test method Methods 0.000 description 3
- 210000001685 thyroid gland Anatomy 0.000 description 3
- 210000003932 urinary bladder Anatomy 0.000 description 3
- LVNGJLRDBYCPGB-LDLOPFEMSA-N (R)-1,2-distearoylphosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[NH3+])OC(=O)CCCCCCCCCCCCCCCCC LVNGJLRDBYCPGB-LDLOPFEMSA-N 0.000 description 2
- DYCJFJRCWPVDHY-UHFFFAOYSA-N 2-(hydroxymethyl)-5-[6-[(4-nitrophenyl)methylsulfanyl]purin-9-yl]oxolane-3,4-diol Chemical compound OC1C(O)C(CO)OC1N1C2=NC=NC(SCC=3C=CC(=CC=3)[N+]([O-])=O)=C2N=C1 DYCJFJRCWPVDHY-UHFFFAOYSA-N 0.000 description 2
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
- NBYLBWHHTUWMER-UHFFFAOYSA-N 2-Methylquinolin-8-ol Chemical compound C1=CC=C(O)C2=NC(C)=CC=C21 NBYLBWHHTUWMER-UHFFFAOYSA-N 0.000 description 2
- FQPDZMRGKXTVSV-UHFFFAOYSA-N 2-[2-(diethylamino)ethylamino]ethanethiol Chemical compound CCN(CC)CCNCCS FQPDZMRGKXTVSV-UHFFFAOYSA-N 0.000 description 2
- FQVAEMASBCTTJN-UHFFFAOYSA-N 2-[4,7-bis(2-sulfanylethyl)-1,4,7-triazonan-1-yl]ethanethiol Chemical compound SCCN1CCN(CCS)CCN(CCS)CC1 FQVAEMASBCTTJN-UHFFFAOYSA-N 0.000 description 2
- UFVLIVCXTIGACT-UHFFFAOYSA-N 2-aminoquinolin-8-ol Chemical compound C1=CC=C(O)C2=NC(N)=CC=C21 UFVLIVCXTIGACT-UHFFFAOYSA-N 0.000 description 2
- MUZDCUCNUGGDMA-UHFFFAOYSA-N 2-benzylquinolin-8-ol Chemical compound N1=C2C(O)=CC=CC2=CC=C1CC1=CC=CC=C1 MUZDCUCNUGGDMA-UHFFFAOYSA-N 0.000 description 2
- MFSHNFBQNVGXJX-UHFFFAOYSA-N 2-oxo-1,2-dihydroquinoline-4-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)=CC(=O)NC2=C1 MFSHNFBQNVGXJX-UHFFFAOYSA-N 0.000 description 2
- HVCOBJNICQPDBP-UHFFFAOYSA-N 3-[3-[3,5-dihydroxy-6-methyl-4-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-2-yl]oxydecanoyloxy]decanoic acid;hydrate Chemical compound O.OC1C(OC(CC(=O)OC(CCCCCCC)CC(O)=O)CCCCCCC)OC(C)C(O)C1OC1C(O)C(O)C(O)C(C)O1 HVCOBJNICQPDBP-UHFFFAOYSA-N 0.000 description 2
- UKWMNFHGYXRSFQ-UHFFFAOYSA-N 5,7-dimethylquinolin-8-ol Chemical compound C1=CC=NC2=C(O)C(C)=CC(C)=C21 UKWMNFHGYXRSFQ-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- YDNKGFDKKRUKPY-JHOUSYSJSA-N C16 ceramide Natural products CCCCCCCCCCCCCCCC(=O)N[C@@H](CO)[C@H](O)C=CCCCCCCCCCCCCC YDNKGFDKKRUKPY-JHOUSYSJSA-N 0.000 description 2
- UGTJLJZQQFGTJD-UHFFFAOYSA-N Carbonylcyanide-3-chlorophenylhydrazone Chemical compound ClC1=CC=CC(NN=C(C#N)C#N)=C1 UGTJLJZQQFGTJD-UHFFFAOYSA-N 0.000 description 2
- 102000020313 Cell-Penetrating Peptides Human genes 0.000 description 2
- 108010051109 Cell-Penetrating Peptides Proteins 0.000 description 2
- QCDFBFJGMNKBDO-UHFFFAOYSA-N Clioquinol Chemical compound C1=CN=C2C(O)=C(I)C=C(Cl)C2=C1 QCDFBFJGMNKBDO-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 2
- 239000005977 Ethylene Substances 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 description 2
- 235000010469 Glycine max Nutrition 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 229910021617 Indium monochloride Inorganic materials 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 239000007987 MES buffer Substances 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- CRJGESKKUOMBCT-VQTJNVASSA-N N-acetylsphinganine Chemical compound CCCCCCCCCCCCCCC[C@@H](O)[C@H](CO)NC(C)=O CRJGESKKUOMBCT-VQTJNVASSA-N 0.000 description 2
- 102000016979 Other receptors Human genes 0.000 description 2
- 208000007452 Plasmacytoma Diseases 0.000 description 2
- 102000005157 Somatostatin Human genes 0.000 description 2
- 108010056088 Somatostatin Proteins 0.000 description 2
- RAOSIAYCXKBGFE-UHFFFAOYSA-K [Cu+3].[O-]P([O-])([O-])=O Chemical compound [Cu+3].[O-]P([O-])([O-])=O RAOSIAYCXKBGFE-UHFFFAOYSA-K 0.000 description 2
- 210000001015 abdomen Anatomy 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000033115 angiogenesis Effects 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- LYMABFPLCIQGMR-UHFFFAOYSA-N benzoic acid;quinolin-8-ol Chemical compound OC(=O)C1=CC=CC=C1.C1=CN=C2C(O)=CC=CC2=C1 LYMABFPLCIQGMR-UHFFFAOYSA-N 0.000 description 2
- 229960000397 bevacizumab Drugs 0.000 description 2
- 239000003124 biologic agent Substances 0.000 description 2
- 239000012620 biological material Substances 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 210000000481 breast Anatomy 0.000 description 2
- 244000309464 bull Species 0.000 description 2
- 210000003169 central nervous system Anatomy 0.000 description 2
- ZVEQCJWYRWKARO-UHFFFAOYSA-N ceramide Natural products CCCCCCCCCCCCCCC(O)C(=O)NC(CO)C(O)C=CCCC=C(C)CCCCCCCCC ZVEQCJWYRWKARO-UHFFFAOYSA-N 0.000 description 2
- 229960005395 cetuximab Drugs 0.000 description 2
- 239000013522 chelant Substances 0.000 description 2
- 210000000038 chest Anatomy 0.000 description 2
- 239000011651 chromium Substances 0.000 description 2
- CTQMJYWDVABFRZ-UHFFFAOYSA-N cloxiquine Chemical compound C1=CN=C2C(O)=CC=C(Cl)C2=C1 CTQMJYWDVABFRZ-UHFFFAOYSA-N 0.000 description 2
- 230000009918 complex formation Effects 0.000 description 2
- 238000010668 complexation reaction Methods 0.000 description 2
- 238000002591 computed tomography Methods 0.000 description 2
- ORTQZVOHEJQUHG-UHFFFAOYSA-L copper(II) chloride Chemical compound Cl[Cu]Cl ORTQZVOHEJQUHG-UHFFFAOYSA-L 0.000 description 2
- SBHDKYTVDCRMOE-JPAPVDFESA-L copper;n'-methyl-n-[(e)-[(3e)-3-[(n-methyl-c-sulfidocarbonimidoyl)hydrazinylidene]butan-2-ylidene]amino]carbamimidothioate Chemical compound [Cu+2].CN=C([S-])N\N=C(/C)\C(\C)=N\NC([S-])=NC SBHDKYTVDCRMOE-JPAPVDFESA-L 0.000 description 2
- QYCVHILLJSYYBD-UHFFFAOYSA-L copper;oxalate Chemical compound [Cu+2].[O-]C(=O)C([O-])=O QYCVHILLJSYYBD-UHFFFAOYSA-L 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 238000000113 differential scanning calorimetry Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 210000000959 ear middle Anatomy 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 210000003238 esophagus Anatomy 0.000 description 2
- 238000001125 extrusion Methods 0.000 description 2
- 239000003925 fat Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000008014 freezing Effects 0.000 description 2
- 238000007710 freezing Methods 0.000 description 2
- 208000015707 frontal fibrosing alopecia Diseases 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 230000003394 haemopoietic effect Effects 0.000 description 2
- 210000003128 head Anatomy 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 238000006703 hydration reaction Methods 0.000 description 2
- 229920001477 hydrophilic polymer Polymers 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 238000010348 incorporation Methods 0.000 description 2
- APHGZSBLRQFRCA-UHFFFAOYSA-M indium(1+);chloride Chemical compound [In]Cl APHGZSBLRQFRCA-UHFFFAOYSA-M 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 230000010220 ion permeability Effects 0.000 description 2
- 210000003734 kidney Anatomy 0.000 description 2
- 238000002372 labelling Methods 0.000 description 2
- 230000001926 lymphatic effect Effects 0.000 description 2
- 239000011572 manganese Substances 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 201000001441 melanoma Diseases 0.000 description 2
- 230000008384 membrane barrier Effects 0.000 description 2
- 150000002739 metals Chemical class 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 210000003739 neck Anatomy 0.000 description 2
- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 description 2
- 210000004798 organs belonging to the digestive system Anatomy 0.000 description 2
- 210000004197 pelvis Anatomy 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- 150000008104 phosphatidylethanolamines Chemical class 0.000 description 2
- 229920000575 polymersome Polymers 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 239000011148 porous material Substances 0.000 description 2
- BNCXJZDIJIVJJO-UHFFFAOYSA-N quinolin-8-ol;sulfuric acid;hydrate Chemical compound O.OS(O)(=O)=O.C1=CN=C2C(O)=CC=CC2=C1.C1=CN=C2C(O)=CC=CC2=C1 BNCXJZDIJIVJJO-UHFFFAOYSA-N 0.000 description 2
- 230000003439 radiotherapeutic effect Effects 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 230000000241 respiratory effect Effects 0.000 description 2
- 230000000717 retained effect Effects 0.000 description 2
- WUAPFZMCVAUBPE-IGMARMGPSA-N rhenium-186 Chemical compound [186Re] WUAPFZMCVAUBPE-IGMARMGPSA-N 0.000 description 2
- 229960004641 rituximab Drugs 0.000 description 2
- VBIZUNYMJSPHBH-OQLLNIDSSA-N salinazid Chemical compound OC1=CC=CC=C1\C=N\NC(=O)C1=CC=NC=C1 VBIZUNYMJSPHBH-OQLLNIDSSA-N 0.000 description 2
- 229950007671 salinazid Drugs 0.000 description 2
- 239000012266 salt solution Substances 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 208000011571 secondary malignant neoplasm Diseases 0.000 description 2
- 229960000553 somatostatin Drugs 0.000 description 2
- 238000001179 sorption measurement Methods 0.000 description 2
- 239000008223 sterile water Substances 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 239000010409 thin film Substances 0.000 description 2
- 229910052723 transition metal Inorganic materials 0.000 description 2
- 150000003624 transition metals Chemical class 0.000 description 2
- 229960000575 trastuzumab Drugs 0.000 description 2
- 230000002485 urinary effect Effects 0.000 description 2
- 230000002792 vascular Effects 0.000 description 2
- BQPPJGMMIYJVBR-UHFFFAOYSA-N (10S)-3c-Acetoxy-4.4.10r.13c.14t-pentamethyl-17c-((R)-1.5-dimethyl-hexen-(4)-yl)-(5tH)-Delta8-tetradecahydro-1H-cyclopenta[a]phenanthren Natural products CC12CCC(OC(C)=O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C BQPPJGMMIYJVBR-UHFFFAOYSA-N 0.000 description 1
- OILXMJHPFNGGTO-UHFFFAOYSA-N (22E)-(24xi)-24-methylcholesta-5,22-dien-3beta-ol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(C)C(C)C)C1(C)CC2 OILXMJHPFNGGTO-UHFFFAOYSA-N 0.000 description 1
- RQOCXCFLRBRBCS-UHFFFAOYSA-N (22E)-cholesta-5,7,22-trien-3beta-ol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CCC(C)C)CCC33)C)C3=CC=C21 RQOCXCFLRBRBCS-UHFFFAOYSA-N 0.000 description 1
- WPWJFABXGZAMQI-SFHVURJKSA-N (2s)-2-(hexadecanoylamino)-4-sulfanylbutanoic acid Chemical compound CCCCCCCCCCCCCCCC(=O)N[C@H](C(O)=O)CCS WPWJFABXGZAMQI-SFHVURJKSA-N 0.000 description 1
- CHGIKSSZNBCNDW-UHFFFAOYSA-N (3beta,5alpha)-4,4-Dimethylcholesta-8,24-dien-3-ol Natural products CC12CCC(O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21 CHGIKSSZNBCNDW-UHFFFAOYSA-N 0.000 description 1
- UNJJBGNPUUVVFQ-NXEZZACHSA-N 1,2-Distearoyl phosphatidyl serine Chemical compound CCCC(=O)O[C@H](COC(=O)CC)COP(O)(=O)OC[C@@H](N)C(O)=O UNJJBGNPUUVVFQ-NXEZZACHSA-N 0.000 description 1
- CITHEXJVPOWHKC-UUWRZZSWSA-N 1,2-di-O-myristoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCC CITHEXJVPOWHKC-UUWRZZSWSA-N 0.000 description 1
- SLKDGVPOSSLUAI-PGUFJCEWSA-N 1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine zwitterion Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OCCN)OC(=O)CCCCCCCCCCCCCCC SLKDGVPOSSLUAI-PGUFJCEWSA-N 0.000 description 1
- KLFKZIQAIPDJCW-GPOMZPHUSA-N 1,2-dihexadecanoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCCCCCCCCCC KLFKZIQAIPDJCW-GPOMZPHUSA-N 0.000 description 1
- PORPENFLTBBHSG-MGBGTMOVSA-N 1,2-dihexadecanoyl-sn-glycerol-3-phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=O)OC(=O)CCCCCCCCCCCCCCC PORPENFLTBBHSG-MGBGTMOVSA-N 0.000 description 1
- WTBFLCSPLLEDEM-JIDRGYQWSA-N 1,2-dioleoyl-sn-glycero-3-phospho-L-serine Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC WTBFLCSPLLEDEM-JIDRGYQWSA-N 0.000 description 1
- BIABMEZBCHDPBV-MPQUPPDSSA-N 1,2-palmitoyl-sn-glycero-3-phospho-(1'-sn-glycerol) Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@@H](O)CO)OC(=O)CCCCCCCCCCCCCCC BIABMEZBCHDPBV-MPQUPPDSSA-N 0.000 description 1
- RUAUPNFNQOGIFF-UHFFFAOYSA-N 1-(4-tert-butyl-2,5-dimethoxyphenyl)propan-2-amine Chemical compound COC1=CC(C(C)(C)C)=C(OC)C=C1CC(C)N RUAUPNFNQOGIFF-UHFFFAOYSA-N 0.000 description 1
- RYCNUMLMNKHWPZ-SNVBAGLBSA-N 1-acetyl-sn-glycero-3-phosphocholine Chemical compound CC(=O)OC[C@@H](O)COP([O-])(=O)OCC[N+](C)(C)C RYCNUMLMNKHWPZ-SNVBAGLBSA-N 0.000 description 1
- ILJAXXNZNFOOQA-DAQGAKHBSA-N 1-oleoyl-2-palmitoyl-sn-glycero-3-phospho-L-serine Chemical compound CCCCCCCCCCCCCCCC(=O)O[C@@H](COP(O)(=O)OC[C@H](N)C(O)=O)COC(=O)CCCCCCC\C=C/CCCCCCCC ILJAXXNZNFOOQA-DAQGAKHBSA-N 0.000 description 1
- FHQVHHIBKUMWTI-ZCXUNETKSA-N 1-palmitoyl-2-oleoyl phosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCCN)OC(=O)CCCCCCC\C=C/CCCCCCCC FHQVHHIBKUMWTI-ZCXUNETKSA-N 0.000 description 1
- PAZGBAOHGQRCBP-DDDNOICHSA-N 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OCC(O)CO)OC(=O)CCCCCCC\C=C/CCCCCCCC PAZGBAOHGQRCBP-DDDNOICHSA-N 0.000 description 1
- AJFWREUFUPEYII-PAHWMLEVSA-N 1-stearoyl-2-oleoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC AJFWREUFUPEYII-PAHWMLEVSA-N 0.000 description 1
- ZPDQFUYPBVXUKS-YADHBBJMSA-N 1-stearoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(O)(=O)OC[C@H](N)C(O)=O ZPDQFUYPBVXUKS-YADHBBJMSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- XYTLYKGXLMKYMV-UHFFFAOYSA-N 14alpha-methylzymosterol Natural products CC12CCC(O)CC1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C XYTLYKGXLMKYMV-UHFFFAOYSA-N 0.000 description 1
- LDGWQMRUWMSZIU-LQDDAWAPSA-M 2,3-bis[(z)-octadec-9-enoxy]propyl-trimethylazanium;chloride Chemical compound [Cl-].CCCCCCCC\C=C/CCCCCCCCOCC(C[N+](C)(C)C)OCCCCCCCC\C=C/CCCCCCCC LDGWQMRUWMSZIU-LQDDAWAPSA-M 0.000 description 1
- UFBJCMHMOXMLKC-UHFFFAOYSA-N 2,4-dinitrophenol Chemical compound OC1=CC=C([N+]([O-])=O)C=C1[N+]([O-])=O UFBJCMHMOXMLKC-UHFFFAOYSA-N 0.000 description 1
- AAKIGGBIGGAVBG-UHFFFAOYSA-N 2-(1,4,8,11-tetrathiacyclotetradec-6-yloxy)hexanoic acid Chemical compound C1(CSCCSCCCSCCSC1)OC(C(=O)O)CCCC.S1CCSCC(CSCCSCCC1)OC(C(=O)O)CCCC AAKIGGBIGGAVBG-UHFFFAOYSA-N 0.000 description 1
- SXGZJKUKBWWHRA-UHFFFAOYSA-N 2-(N-morpholiniumyl)ethanesulfonate Chemical compound [O-]S(=O)(=O)CC[NH+]1CCOCC1 SXGZJKUKBWWHRA-UHFFFAOYSA-N 0.000 description 1
- XMLFIOJWWQQWAH-UHFFFAOYSA-N 2-[(1-carboxy-2-methylpropyl)amino]-3-methylbutanoic acid Chemical compound CC(C)C(C(O)=O)NC(C(C)C)C(O)=O XMLFIOJWWQQWAH-UHFFFAOYSA-N 0.000 description 1
- SQCRCKFOMCLOGC-UHFFFAOYSA-N 2-[2-(diethylamino)ethyl-(2-sulfanylethyl)amino]ethanethiol Chemical compound CCN(CC)CCN(CCS)CCS SQCRCKFOMCLOGC-UHFFFAOYSA-N 0.000 description 1
- UKLVPVPGVSSSIB-UHFFFAOYSA-N 2-[2-[2-(dioctadecylamino)-2-oxoethoxy]ethoxy]-n,n-dipropylacetamide Chemical compound CCCCCCCCCCCCCCCCCCN(C(=O)COCCOCC(=O)N(CCC)CCC)CCCCCCCCCCCCCCCCCC UKLVPVPGVSSSIB-UHFFFAOYSA-N 0.000 description 1
- FTGBVHPWUIHWRH-UHFFFAOYSA-N 2-[2-[2-[2-[carboxymethyl-[2-(2-octoxyethoxy)-2-oxoethyl]amino]phenoxy]ethoxy]-n-[2-(2-octoxyethoxy)-2-oxoethyl]anilino]acetic acid Chemical compound CCCCCCCCOCCOC(=O)CN(CC(O)=O)C1=CC=CC=C1OCCOC1=CC=CC=C1N(CC(O)=O)CC(=O)OCCOCCCCCCCC FTGBVHPWUIHWRH-UHFFFAOYSA-N 0.000 description 1
- VGCOGXWEJYLXMQ-UHFFFAOYSA-N 2-[8-(carboxymethyl)-1,4,8,11-tetrazacyclotetradec-1-yl]acetic acid Chemical compound OC(=O)CN1CCCNCCN(CC(O)=O)CCCNCC1 VGCOGXWEJYLXMQ-UHFFFAOYSA-N 0.000 description 1
- NEZDNQCXEZDCBI-UHFFFAOYSA-N 2-azaniumylethyl 2,3-di(tetradecanoyloxy)propyl phosphate Chemical compound CCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCCN)OC(=O)CCCCCCCCCCCCC NEZDNQCXEZDCBI-UHFFFAOYSA-N 0.000 description 1
- MPNXSZJPSVBLHP-UHFFFAOYSA-N 2-chloro-n-phenylpyridine-3-carboxamide Chemical compound ClC1=NC=CC=C1C(=O)NC1=CC=CC=C1 MPNXSZJPSVBLHP-UHFFFAOYSA-N 0.000 description 1
- HNUFDBQIXGQAEX-UHFFFAOYSA-N 2-chloroquinolin-8-ol Chemical compound C1=C(Cl)N=C2C(O)=CC=CC2=C1 HNUFDBQIXGQAEX-UHFFFAOYSA-N 0.000 description 1
- VKHPNLQKEJLIPJ-UHFFFAOYSA-N 2-chloroquinolin-8-ol;hydrochloride Chemical compound Cl.C1=C(Cl)N=C2C(O)=CC=CC2=C1 VKHPNLQKEJLIPJ-UHFFFAOYSA-N 0.000 description 1
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 description 1
- FPTJELQXIUUCEY-UHFFFAOYSA-N 3beta-Hydroxy-lanostan Natural products C1CC2C(C)(C)C(O)CCC2(C)C2C1C1(C)CCC(C(C)CCCC(C)C)C1(C)CC2 FPTJELQXIUUCEY-UHFFFAOYSA-N 0.000 description 1
- LAQRPDPJOOMNHB-UHFFFAOYSA-N 4,6-dimethyl-1h-quinolin-2-one Chemical compound N1C(=O)C=C(C)C2=CC(C)=CC=C21 LAQRPDPJOOMNHB-UHFFFAOYSA-N 0.000 description 1
- NJUAEGGYLOZMGV-UHFFFAOYSA-N 4,8-dimethyl-1h-quinolin-2-one Chemical compound C1=CC=C2C(C)=CC(=O)NC2=C1C NJUAEGGYLOZMGV-UHFFFAOYSA-N 0.000 description 1
- ZDASUJMDVPTNTF-UHFFFAOYSA-N 5,7-dibromo-8-quinolinol Chemical compound C1=CN=C2C(O)=C(Br)C=C(Br)C2=C1 ZDASUJMDVPTNTF-UHFFFAOYSA-N 0.000 description 1
- HIYAVKIYRIFSCZ-CYEMHPAKSA-N 5-(methylamino)-2-[[(2S,3R,5R,6S,8R,9R)-3,5,9-trimethyl-2-[(2S)-1-oxo-1-(1H-pyrrol-2-yl)propan-2-yl]-1,7-dioxaspiro[5.5]undecan-8-yl]methyl]-1,3-benzoxazole-4-carboxylic acid Chemical compound O=C([C@@H](C)[C@H]1O[C@@]2([C@@H](C[C@H]1C)C)O[C@@H]([C@@H](CC2)C)CC=1OC2=CC=C(C(=C2N=1)C(O)=O)NC)C1=CC=CN1 HIYAVKIYRIFSCZ-CYEMHPAKSA-N 0.000 description 1
- TURFSTYEMSSDCV-UHFFFAOYSA-N 5-amino-1,3-diethyl-6-methylbenzimidazol-2-one Chemical compound CC1=C(N)C=C2N(CC)C(=O)N(CC)C2=C1 TURFSTYEMSSDCV-UHFFFAOYSA-N 0.000 description 1
- QKWIORGVGGOEFG-UHFFFAOYSA-N 5-chloroquinolin-8-ol;hydrochloride Chemical compound Cl.C1=CN=C2C(O)=CC=C(Cl)C2=C1 QKWIORGVGGOEFG-UHFFFAOYSA-N 0.000 description 1
- OJEBWFGRUPIVSD-UHFFFAOYSA-N 6-chloro-1h-quinolin-2-one Chemical compound C1=C(Cl)C=CC2=NC(O)=CC=C21 OJEBWFGRUPIVSD-UHFFFAOYSA-N 0.000 description 1
- HBBSDZXXUIHKJE-UHFFFAOYSA-N 6-hydrazinylpyridine-3-carboxylic acid Chemical compound NNC1=CC=C(C(O)=O)C=N1 HBBSDZXXUIHKJE-UHFFFAOYSA-N 0.000 description 1
- LHWKOWLGYNIFSM-UHFFFAOYSA-N 7-(dimethylamino)-4-methyl-1h-quinolin-2-one Chemical compound CC1=CC(=O)NC2=CC(N(C)C)=CC=C21 LHWKOWLGYNIFSM-UHFFFAOYSA-N 0.000 description 1
- OQMZNAMGEHIHNN-UHFFFAOYSA-N 7-Dehydrostigmasterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CC(CC)C(C)C)CCC33)C)C3=CC=C21 OQMZNAMGEHIHNN-UHFFFAOYSA-N 0.000 description 1
- MJXYFLJHTUSJGU-UHFFFAOYSA-N 7-amino-4-methyl-1h-quinolin-2-one Chemical compound NC1=CC=C2C(C)=CC(=O)NC2=C1 MJXYFLJHTUSJGU-UHFFFAOYSA-N 0.000 description 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 1
- 108010009551 Alamethicin Proteins 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 208000012791 Alpha-heavy chain disease Diseases 0.000 description 1
- USFZMSVCRYTOJT-UHFFFAOYSA-N Ammonium acetate Chemical compound N.CC(O)=O USFZMSVCRYTOJT-UHFFFAOYSA-N 0.000 description 1
- 239000005695 Ammonium acetate Substances 0.000 description 1
- FTEDXVNDVHYDQW-UHFFFAOYSA-N BAPTA Chemical compound OC(=O)CN(CC(O)=O)C1=CC=CC=C1OCCOC1=CC=CC=C1N(CC(O)=O)CC(O)=O FTEDXVNDVHYDQW-UHFFFAOYSA-N 0.000 description 1
- 208000008720 Bone Marrow Neoplasms Diseases 0.000 description 1
- 208000018084 Bone neoplasm Diseases 0.000 description 1
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical compound [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 description 1
- 241001260012 Bursa Species 0.000 description 1
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 1
- CLSRDUAWSNUIHN-UHFFFAOYSA-N CC(C)CN(CC(C)C)C([SH2]CC1=CC=CC=C1C[SH2]C(N(CC(C)C)CC(C)C)=S)=S Chemical compound CC(C)CN(CC(C)C)C([SH2]CC1=CC=CC=C1C[SH2]C(N(CC(C)C)CC(C)C)=S)=S CLSRDUAWSNUIHN-UHFFFAOYSA-N 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 108010001857 Cell Surface Receptors Proteins 0.000 description 1
- CXRFDZFCGOPDTD-UHFFFAOYSA-M Cetrimide Chemical compound [Br-].CCCCCCCCCCCCCC[N+](C)(C)C CXRFDZFCGOPDTD-UHFFFAOYSA-M 0.000 description 1
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 description 1
- BHYOQNUELFTYRT-UHFFFAOYSA-N Cholesterol sulfate Natural products C1C=C2CC(OS(O)(=O)=O)CCC2(C)C2C1C1CCC(C(C)CCCC(C)C)C1(C)CC2 BHYOQNUELFTYRT-UHFFFAOYSA-N 0.000 description 1
- JPVYNHNXODAKFH-UHFFFAOYSA-N Cu2+ Chemical compound [Cu+2] JPVYNHNXODAKFH-UHFFFAOYSA-N 0.000 description 1
- 108010069514 Cyclic Peptides Proteins 0.000 description 1
- 102000001189 Cyclic Peptides Human genes 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- MNQZXJOMYWMBOU-VKHMYHEASA-N D-glyceraldehyde Chemical compound OC[C@@H](O)C=O MNQZXJOMYWMBOU-VKHMYHEASA-N 0.000 description 1
- 108010074327 DECYL-2 Proteins 0.000 description 1
- 108010002156 Depsipeptides Proteins 0.000 description 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- DNVPQKQSNYMLRS-NXVQYWJNSA-N Ergosterol Natural products CC(C)[C@@H](C)C=C[C@H](C)[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)CC[C@]4(C)[C@@H]3CC[C@]12C DNVPQKQSNYMLRS-NXVQYWJNSA-N 0.000 description 1
- BPNZYADGDZPRTK-UDUYQYQQSA-N Exametazime Chemical compound O/N=C(\C)[C@@H](C)NCC(C)(C)CN[C@H](C)C(\C)=N\O BPNZYADGDZPRTK-UDUYQYQQSA-N 0.000 description 1
- 206010015866 Extravasation Diseases 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 208000012841 Gamma-heavy chain disease Diseases 0.000 description 1
- BKLIAINBCQPSOV-UHFFFAOYSA-N Gluanol Natural products CC(C)CC=CC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(O)C(C)(C)C4CC3 BKLIAINBCQPSOV-UHFFFAOYSA-N 0.000 description 1
- ZWZWYGMENQVNFU-UHFFFAOYSA-N Glycerophosphorylserin Natural products OC(=O)C(N)COP(O)(=O)OCC(O)CO ZWZWYGMENQVNFU-UHFFFAOYSA-N 0.000 description 1
- 244000068988 Glycine max Species 0.000 description 1
- 108010026389 Gramicidin Proteins 0.000 description 1
- 208000017604 Hodgkin disease Diseases 0.000 description 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 description 1
- 206010062767 Hypophysitis Diseases 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- LOPKHWOTGJIQLC-UHFFFAOYSA-N Lanosterol Natural products CC(CCC=C(C)C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 LOPKHWOTGJIQLC-UHFFFAOYSA-N 0.000 description 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
- 206010024305 Leukaemia monocytic Diseases 0.000 description 1
- 208000028018 Lymphocytic leukaemia Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010025638 Malignant mast cell neoplasm Diseases 0.000 description 1
- 206010061272 Malignant urinary tract neoplasm Diseases 0.000 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 206010027407 Mesothelioma malignant Diseases 0.000 description 1
- GAOZTHIDHYLHMS-UHFFFAOYSA-N Monensin A Natural products O1C(CC)(C2C(CC(O2)C2C(CC(C)C(O)(CO)O2)C)C)CCC1C(O1)(C)CCC21CC(O)C(C)C(C(C)C(OC)C(C)C(O)=O)O2 GAOZTHIDHYLHMS-UHFFFAOYSA-N 0.000 description 1
- CAHGCLMLTWQZNJ-UHFFFAOYSA-N Nerifoliol Natural products CC12CCC(O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C CAHGCLMLTWQZNJ-UHFFFAOYSA-N 0.000 description 1
- RMIXHJPMNBXMBU-QIIXEHPYSA-N Nonactin Chemical compound C[C@H]([C@H]1CC[C@H](O1)C[C@@H](OC(=O)[C@@H](C)[C@@H]1CC[C@@H](O1)C[C@@H](C)OC(=O)[C@H](C)[C@H]1CC[C@H](O1)C[C@H](C)OC(=O)[C@H]1C)C)C(=O)O[C@H](C)C[C@H]2CC[C@@H]1O2 RMIXHJPMNBXMBU-QIIXEHPYSA-N 0.000 description 1
- RMIXHJPMNBXMBU-UHFFFAOYSA-N Nonactin Natural products CC1C(=O)OC(C)CC(O2)CCC2C(C)C(=O)OC(C)CC(O2)CCC2C(C)C(=O)OC(C)CC(O2)CCC2C(C)C(=O)OC(C)CC2CCC1O2 RMIXHJPMNBXMBU-UHFFFAOYSA-N 0.000 description 1
- 108010077850 Nuclear Localization Signals Proteins 0.000 description 1
- 108010078678 Osmolite Proteins 0.000 description 1
- 101710160107 Outer membrane protein A Proteins 0.000 description 1
- 238000012879 PET imaging Methods 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 206010061336 Pelvic neoplasm Diseases 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- KQXDHUJYNAXLNZ-XQSDOZFQSA-N Salinomycin Chemical compound O1[C@@H]([C@@H](CC)C(O)=O)CC[C@H](C)[C@@H]1[C@@H](C)[C@H](O)[C@H](C)C(=O)[C@H](CC)[C@@H]1[C@@H](C)C[C@@H](C)[C@@]2(C=C[C@@H](O)[C@@]3(O[C@@](C)(CC3)[C@@H]3O[C@@H](C)[C@@](O)(CC)CC3)O2)O1 KQXDHUJYNAXLNZ-XQSDOZFQSA-N 0.000 description 1
- 239000004189 Salinomycin Substances 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 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 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- GKLVYJBZJHMRIY-OUBTZVSYSA-N Technetium-99 Chemical compound [99Tc] GKLVYJBZJHMRIY-OUBTZVSYSA-N 0.000 description 1
- 108010067973 Valinomycin Proteins 0.000 description 1
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 description 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 description 1
- CWRILEGKIAOYKP-SSDOTTSWSA-M [(2r)-3-acetyloxy-2-hydroxypropyl] 2-aminoethyl phosphate Chemical compound CC(=O)OC[C@@H](O)COP([O-])(=O)OCCN CWRILEGKIAOYKP-SSDOTTSWSA-M 0.000 description 1
- JLPULHDHAOZNQI-JLOPVYAASA-N [(2r)-3-hexadecanoyloxy-2-[(9e,12e)-octadeca-9,12-dienoyl]oxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical class CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C\C\C=C\CCCCC JLPULHDHAOZNQI-JLOPVYAASA-N 0.000 description 1
- RRVPPYNAZJRZFR-MRCUWXFGSA-N [2-hexadecanoyloxy-3-[(z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCC\C=C/CCCCCCCC RRVPPYNAZJRZFR-MRCUWXFGSA-N 0.000 description 1
- NMJCSTNQFYPVOR-XDOYNYLZSA-N [2-octadecanoyloxy-3-[(z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC(COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCC\C=C/CCCCCCCC NMJCSTNQFYPVOR-XDOYNYLZSA-N 0.000 description 1
- DSNRWDQKZIEDDB-UHFFFAOYSA-N [3-[2,3-dihydroxypropoxy(hydroxy)phosphoryl]oxy-2-octadec-9-enoyloxypropyl] octadec-9-enoate Chemical compound CCCCCCCCC=CCCCCCCCC(=O)OCC(COP(O)(=O)OCC(O)CO)OC(=O)CCCCCCCC=CCCCCCCCC DSNRWDQKZIEDDB-UHFFFAOYSA-N 0.000 description 1
- ATHVAWFAEPLPPQ-LNVKXUELSA-N [3-octadecanoyloxy-2-[(z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/CCCCCCCC ATHVAWFAEPLPPQ-LNVKXUELSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 208000036676 acute undifferentiated leukemia Diseases 0.000 description 1
- 230000001919 adrenal effect Effects 0.000 description 1
- 210000004100 adrenal gland Anatomy 0.000 description 1
- LGHSQOCGTJHDIL-UTXLBGCNSA-N alamethicin Chemical compound N([C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)CC=1C=CC=CC=1)C(C)C)C(=O)C(C)(C)NC(=O)[C@@H]1CCCN1C(=O)C(C)(C)NC(C)=O LGHSQOCGTJHDIL-UTXLBGCNSA-N 0.000 description 1
- 238000005904 alkaline hydrolysis reaction Methods 0.000 description 1
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 229940043376 ammonium acetate Drugs 0.000 description 1
- 235000019257 ammonium acetate Nutrition 0.000 description 1
- 210000002255 anal canal Anatomy 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 150000001450 anions Chemical class 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000000427 antigen Substances 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 210000002413 aortic body Anatomy 0.000 description 1
- PYMYPHUHKUWMLA-WDCZJNDASA-N arabinose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)C=O PYMYPHUHKUWMLA-WDCZJNDASA-N 0.000 description 1
- PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 238000001636 atomic emission spectroscopy Methods 0.000 description 1
- 230000002567 autonomic effect Effects 0.000 description 1
- 125000000656 azaniumyl group Chemical group [H][N+]([H])([H])[*] 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 108010079684 beauvericin Proteins 0.000 description 1
- GYSCAQFHASJXRS-FFCOJMSVSA-N beauvericin Chemical compound C([C@H]1C(=O)O[C@@H](C(N(C)[C@@H](CC=2C=CC=CC=2)C(=O)O[C@@H](C(=O)N(C)[C@@H](CC=2C=CC=CC=2)C(=O)O[C@@H](C(=O)N1C)C(C)C)C(C)C)=O)C(C)C)C1=CC=CC=C1 GYSCAQFHASJXRS-FFCOJMSVSA-N 0.000 description 1
- GYSCAQFHASJXRS-UHFFFAOYSA-N beauvericin Natural products CN1C(=O)C(C(C)C)OC(=O)C(CC=2C=CC=CC=2)N(C)C(=O)C(C(C)C)OC(=O)C(CC=2C=CC=CC=2)N(C)C(=O)C(C(C)C)OC(=O)C1CC1=CC=CC=C1 GYSCAQFHASJXRS-UHFFFAOYSA-N 0.000 description 1
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 230000001588 bifunctional effect Effects 0.000 description 1
- 210000003445 biliary tract Anatomy 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- 201000006491 bone marrow cancer Diseases 0.000 description 1
- 210000003557 bones of lower extremity Anatomy 0.000 description 1
- 229910052796 boron Inorganic materials 0.000 description 1
- 210000000621 bronchi Anatomy 0.000 description 1
- DEGAKNSWVGKMLS-UHFFFAOYSA-N calcein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC(CN(CC(O)=O)CC(O)=O)=C(O)C=C1OC1=C2C=C(CN(CC(O)=O)CC(=O)O)C(O)=C1 DEGAKNSWVGKMLS-UHFFFAOYSA-N 0.000 description 1
- 125000002843 carboxylic acid group Chemical group 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 210000001011 carotid body Anatomy 0.000 description 1
- 210000000845 cartilage Anatomy 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 210000003679 cervix uteri Anatomy 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 150000004697 chelate complex Chemical class 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- BHYOQNUELFTYRT-DPAQBDIFSA-N cholesterol sulfate Chemical compound C1C=C2C[C@@H](OS(O)(=O)=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 BHYOQNUELFTYRT-DPAQBDIFSA-N 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 230000000536 complexating effect Effects 0.000 description 1
- FCFNRCROJUBPLU-UHFFFAOYSA-N compound M126 Natural products CC(C)C1NC(=O)C(C)OC(=O)C(C(C)C)NC(=O)C(C(C)C)OC(=O)C(C(C)C)NC(=O)C(C)OC(=O)C(C(C)C)NC(=O)C(C(C)C)OC(=O)C(C(C)C)NC(=O)C(C)OC(=O)C(C(C)C)NC(=O)C(C(C)C)OC1=O FCFNRCROJUBPLU-UHFFFAOYSA-N 0.000 description 1
- 230000003750 conditioning effect Effects 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 239000002872 contrast media Substances 0.000 description 1
- 229910001431 copper ion Inorganic materials 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 210000003792 cranial nerve Anatomy 0.000 description 1
- 238000009109 curative therapy Methods 0.000 description 1
- 208000030381 cutaneous melanoma Diseases 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000010537 deprotonation reaction Methods 0.000 description 1
- 238000003795 desorption Methods 0.000 description 1
- 230000000368 destabilizing effect Effects 0.000 description 1
- 230000001066 destructive effect Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 238000002059 diagnostic imaging Methods 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- YSSSPARMOAYJTE-UHFFFAOYSA-N dibenzo-18-crown-6 Chemical compound O1CCOCCOC2=CC=CC=C2OCCOCCOC2=CC=CC=C21 YSSSPARMOAYJTE-UHFFFAOYSA-N 0.000 description 1
- 229920000359 diblock copolymer Polymers 0.000 description 1
- QBSJHOGDIUQWTH-UHFFFAOYSA-N dihydrolanosterol Natural products CC(C)CCCC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 QBSJHOGDIUQWTH-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000010494 dissociation reaction Methods 0.000 description 1
- 230000005593 dissociations Effects 0.000 description 1
- XJWSAJYUBXQQDR-UHFFFAOYSA-M dodecyltrimethylammonium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)C XJWSAJYUBXQQDR-UHFFFAOYSA-M 0.000 description 1
- 238000003411 electrode reaction Methods 0.000 description 1
- 230000009881 electrostatic interaction Effects 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 210000003372 endocrine gland Anatomy 0.000 description 1
- 230000012202 endocytosis Effects 0.000 description 1
- MIZMDSVSLSIMSC-OGLSAIDSSA-N enniatin Chemical compound CC(C)C1OC(=O)[C@H](C(C)C)N(C)C(=O)C(C(C)C)OC(=O)[C@H](C(C)C)N(C)C(=O)C(C(C)C)OC(=O)[C@H](C(C)C)N(C)C1=O MIZMDSVSLSIMSC-OGLSAIDSSA-N 0.000 description 1
- 229930191716 enniatin Natural products 0.000 description 1
- DANUORFCFTYTSZ-UHFFFAOYSA-N epinigericin Natural products O1C2(C(CC(C)(O2)C2OC(C)(CC2)C2C(CC(O2)C2C(CC(C)C(O)(CO)O2)C)C)C)C(C)C(OC)CC1CC1CCC(C)C(C(C)C(O)=O)O1 DANUORFCFTYTSZ-UHFFFAOYSA-N 0.000 description 1
- DNVPQKQSNYMLRS-SOWFXMKYSA-N ergosterol Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H](CC[C@]3([C@H]([C@H](C)/C=C/[C@@H](C)C(C)C)CC[C@H]33)C)C3=CC=C21 DNVPQKQSNYMLRS-SOWFXMKYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 230000036251 extravasation Effects 0.000 description 1
- 210000003195 fascia Anatomy 0.000 description 1
- 150000002191 fatty alcohols Chemical class 0.000 description 1
- 239000010408 film Substances 0.000 description 1
- 201000003444 follicular lymphoma Diseases 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 210000000232 gallbladder Anatomy 0.000 description 1
- QPJBWNIQKHGLAU-IQZHVAEDSA-N ganglioside GM1 Chemical compound O[C@@H]1[C@@H](O)[C@H](OC[C@H](NC(=O)CCCCCCCCCCCCCCCCC)[C@H](O)\C=C\CCCCCCCCCCCCC)O[C@H](CO)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@]2(O[C@H]([C@H](NC(C)=O)[C@@H](O)C2)[C@H](O)[C@H](O)CO)C(O)=O)[C@@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O3)O)[C@@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](CO)O1 QPJBWNIQKHGLAU-IQZHVAEDSA-N 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 229960004905 gramicidin Drugs 0.000 description 1
- ZWCXYZRRTRDGQE-SORVKSEFSA-N gramicidina Chemical compound C1=CC=C2C(C[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC=O)C(C)C)CC(C)C)C(=O)NCCO)=CNC2=C1 ZWCXYZRRTRDGQE-SORVKSEFSA-N 0.000 description 1
- 230000000887 hydrating effect Effects 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- XLSMFKSTNGKWQX-UHFFFAOYSA-N hydroxyacetone Chemical compound CC(=O)CO XLSMFKSTNGKWQX-UHFFFAOYSA-N 0.000 description 1
- 230000007954 hypoxia Effects 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 208000025095 immunoproliferative disease Diseases 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 210000003228 intrahepatic bile duct Anatomy 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- PGHMRUGBZOYCAA-ADZNBVRBSA-N ionomycin Chemical compound O1[C@H](C[C@H](O)[C@H](C)[C@H](O)[C@H](C)/C=C/C[C@@H](C)C[C@@H](C)C(/O)=C/C(=O)[C@@H](C)C[C@@H](C)C[C@@H](CCC(O)=O)C)CC[C@@]1(C)[C@@H]1O[C@](C)([C@@H](C)O)CC1 PGHMRUGBZOYCAA-ADZNBVRBSA-N 0.000 description 1
- PGHMRUGBZOYCAA-UHFFFAOYSA-N ionomycin Natural products O1C(CC(O)C(C)C(O)C(C)C=CCC(C)CC(C)C(O)=CC(=O)C(C)CC(C)CC(CCC(O)=O)C)CCC1(C)C1OC(C)(C(C)O)CC1 PGHMRUGBZOYCAA-UHFFFAOYSA-N 0.000 description 1
- 210000005067 joint tissue Anatomy 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- CAHGCLMLTWQZNJ-RGEKOYMOSA-N lanosterol Chemical compound C([C@]12C)C[C@@H](O)C(C)(C)[C@H]1CCC1=C2CC[C@]2(C)[C@H]([C@H](CCC=C(C)C)C)CC[C@@]21C CAHGCLMLTWQZNJ-RGEKOYMOSA-N 0.000 description 1
- 229940058690 lanosterol Drugs 0.000 description 1
- 210000000867 larynx Anatomy 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 210000003041 ligament Anatomy 0.000 description 1
- 239000004973 liquid crystal related substance Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 210000002751 lymph Anatomy 0.000 description 1
- 210000001165 lymph node Anatomy 0.000 description 1
- 210000004324 lymphatic system Anatomy 0.000 description 1
- 208000003747 lymphoid leukemia Diseases 0.000 description 1
- 208000025036 lymphosarcoma Diseases 0.000 description 1
- 229920001427 mPEG Polymers 0.000 description 1
- 150000002678 macrocyclic compounds Chemical group 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 208000016847 malignant urinary system neoplasm Diseases 0.000 description 1
- 239000003550 marker Substances 0.000 description 1
- 210000002418 meninge Anatomy 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 201000006894 monocytic leukemia Diseases 0.000 description 1
- 101150085329 mrp20 gene Proteins 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 208000025113 myeloid leukemia Diseases 0.000 description 1
- 201000000050 myeloid neoplasm Diseases 0.000 description 1
- URAUKAJXWWFQSU-UHFFFAOYSA-N n,n-dicyclohexyl-2-[2-(dicyclohexylamino)-2-oxoethoxy]acetamide Chemical compound C1CCCCC1N(C1CCCCC1)C(=O)COCC(=O)N(C1CCCCC1)C1CCCCC1 URAUKAJXWWFQSU-UHFFFAOYSA-N 0.000 description 1
- BUESTOLSNRTEQW-UHFFFAOYSA-N n,n-dicyclohexyl-2-[2-(dicyclohexylamino)-2-oxoethyl]sulfanylacetamide Chemical compound C1CCCCC1N(C1CCCCC1)C(=O)CSCC(=O)N(C1CCCCC1)C1CCCCC1 BUESTOLSNRTEQW-UHFFFAOYSA-N 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 210000001989 nasopharynx Anatomy 0.000 description 1
- 230000009826 neoplastic cell growth Effects 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- DANUORFCFTYTSZ-BIBFWWMMSA-N nigericin Chemical compound C([C@@H]1C[C@H]([C@H]([C@]2([C@@H](C[C@](C)(O2)C2O[C@@](C)(CC2)C2[C@H](CC(O2)[C@@H]2[C@H](C[C@@H](C)[C@](O)(CO)O2)C)C)C)O1)C)OC)[C@H]1CC[C@H](C)C([C@@H](C)C(O)=O)O1 DANUORFCFTYTSZ-BIBFWWMMSA-N 0.000 description 1
- 230000030648 nucleus localization Effects 0.000 description 1
- 229960000988 nystatin Drugs 0.000 description 1
- VQOXZBDYSJBXMA-NQTDYLQESA-N nystatin A1 Chemical compound O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/CC/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 VQOXZBDYSJBXMA-NQTDYLQESA-N 0.000 description 1
- CFODQUSMSYDHBS-UHFFFAOYSA-N octreotate Chemical compound O=C1NC(CC=2C=CC=CC=2)C(=O)NC(CC=2[C]3C=CC=CC3=NC=2)C(=O)NC(CCCCN)C(=O)NC(C(C)O)C(=O)NC(C(=O)NC(C(O)C)C(O)=O)CSSCC1NC(=O)C(N)CC1=CC=CC=C1 CFODQUSMSYDHBS-UHFFFAOYSA-N 0.000 description 1
- 229960002378 oftasceine Drugs 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 150000002482 oligosaccharides Chemical class 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 201000005443 oral cavity cancer Diseases 0.000 description 1
- 210000003300 oropharynx Anatomy 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 210000003101 oviduct Anatomy 0.000 description 1
- 150000002923 oximes Chemical class 0.000 description 1
- 238000010979 pH adjustment Methods 0.000 description 1
- 210000003254 palate Anatomy 0.000 description 1
- 210000002741 palatine tonsil Anatomy 0.000 description 1
- 210000002990 parathyroid gland Anatomy 0.000 description 1
- 210000003681 parotid gland Anatomy 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 210000003899 penis Anatomy 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 150000008105 phosphatidylcholines Chemical class 0.000 description 1
- 229940067605 phosphatidylethanolamines Drugs 0.000 description 1
- ZWLUXSQADUDCSB-UHFFFAOYSA-N phthalaldehyde Chemical compound O=CC1=CC=CC=C1C=O ZWLUXSQADUDCSB-UHFFFAOYSA-N 0.000 description 1
- 210000004560 pineal gland Anatomy 0.000 description 1
- 210000003635 pituitary gland Anatomy 0.000 description 1
- 230000003169 placental effect Effects 0.000 description 1
- 208000031223 plasma cell leukemia Diseases 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 description 1
- 229940124606 potential therapeutic agent Drugs 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000002028 premature Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 230000005588 protonation Effects 0.000 description 1
- GYESAYHWISMZOK-UHFFFAOYSA-N quinolin-5-ol Chemical compound C1=CC=C2C(O)=CC=CC2=N1 GYESAYHWISMZOK-UHFFFAOYSA-N 0.000 description 1
- ZVJDFJRDKIADMB-UHFFFAOYSA-N quinolin-8-ol;sodium Chemical compound [Na].C1=CN=C2C(O)=CC=CC2=C1 ZVJDFJRDKIADMB-UHFFFAOYSA-N 0.000 description 1
- KVGSJGNWRDPVKA-UHFFFAOYSA-N quinoline-5-sulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=N1 KVGSJGNWRDPVKA-UHFFFAOYSA-N 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 201000006845 reticulosarcoma Diseases 0.000 description 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 description 1
- 229960001548 salinomycin Drugs 0.000 description 1
- 235000019378 salinomycin Nutrition 0.000 description 1
- 210000003079 salivary gland Anatomy 0.000 description 1
- 210000001732 sebaceous gland Anatomy 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 201000006000 skin carcinoma in situ Diseases 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000003393 splenic effect Effects 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000012086 standard solution Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 239000003351 stiffener Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 210000000106 sweat gland Anatomy 0.000 description 1
- 210000001179 synovial fluid Anatomy 0.000 description 1
- 230000002277 temperature effect Effects 0.000 description 1
- 210000002435 tendon Anatomy 0.000 description 1
- 230000002381 testicular Effects 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- SRVJKTDHMYAMHA-WUXMJOGZSA-N thioacetazone Chemical compound CC(=O)NC1=CC=C(\C=N\NC(N)=S)C=C1 SRVJKTDHMYAMHA-WUXMJOGZSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 231100000820 toxicity test Toxicity 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- 210000003437 trachea Anatomy 0.000 description 1
- 229910001428 transition metal ion Inorganic materials 0.000 description 1
- ILJSQTXMGCGYMG-UHFFFAOYSA-N triacetic acid Chemical compound CC(=O)CC(=O)CC(O)=O ILJSQTXMGCGYMG-UHFFFAOYSA-N 0.000 description 1
- 229920000428 triblock copolymer Polymers 0.000 description 1
- RRBYUSWBLVXTQN-UHFFFAOYSA-N tricyclene Chemical compound C12CC3CC2C1(C)C3(C)C RRBYUSWBLVXTQN-UHFFFAOYSA-N 0.000 description 1
- RRBYUSWBLVXTQN-VZCHMASFSA-N tricyclene Natural products C([C@@H]12)C3C[C@H]1C2(C)C3(C)C RRBYUSWBLVXTQN-VZCHMASFSA-N 0.000 description 1
- 210000000626 ureter Anatomy 0.000 description 1
- 210000003708 urethra Anatomy 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- FCFNRCROJUBPLU-DNDCDFAISA-N valinomycin Chemical compound CC(C)[C@@H]1NC(=O)[C@H](C)OC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C(C)C)OC(=O)[C@H](C(C)C)NC(=O)[C@H](C)OC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C(C)C)OC(=O)[C@H](C(C)C)NC(=O)[C@H](C)OC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C(C)C)OC1=O FCFNRCROJUBPLU-DNDCDFAISA-N 0.000 description 1
- 238000012800 visualization Methods 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 210000003905 vulva Anatomy 0.000 description 1
- OIWCYIUQAVBPGV-DAQGAKHBSA-N {1-O-hexadecanoyl-2-O-[(Z)-octadec-9-enoyl]-sn-glycero-3-phospho}serine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC OIWCYIUQAVBPGV-DAQGAKHBSA-N 0.000 description 1
Images
Classifications
-
- 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
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
- A61K51/1217—Dispersions, suspensions, colloids, emulsions, e.g. perfluorinated emulsion, sols
- A61K51/1234—Liposomes
- A61K51/1237—Polymersomes, i.e. liposomes with polymerisable or polymerized bilayer-forming substances
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
- A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
- A61K51/1203—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules in a form not provided for by groups A61K51/1206 - A61K51/1296, e.g. cells, cell fragments, viruses, virus capsides, ghosts, red blood cells, viral vectors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
- A61K51/1217—Dispersions, suspensions, colloids, emulsions, e.g. perfluorinated emulsion, sols
- A61K51/1234—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
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0404—Lipids, e.g. triglycerides; Polycationic carriers
- A61K51/0408—Phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
Description
リポソーム組成物等のリン脂質二重層の低いイオン透過性(非特許文献17〜22)により、荷電イオン種の封入速度は非常に低くなることが知られている。従って、二重層透過拡散速度を上昇させ、リポソーム等のナノ粒子内への一価、二価及び三価カチオンの封入を向上させるためにイオノフォアが通常使用されている。
a.ベシクル形成成分と、前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物を用意する工程と、
b.前記金属体を含む溶液内において前記ナノ粒子組成物を培養することにより、前記ベシクル形成成分によって形成された膜を透過するカチオン金属体の移動を可能とすることによって前記ナノ粒子組成物の内部に前記金属体を封入する工程と、
を含む。
a.i)ベシクル形成成分と、ii)前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物と、
b.前記ナノ粒子に封入される金属体を含む組成物と、
を含むキット・オブ・パーツを提供する。
i.ベシクル形成成分と、
ii.前記ベシクル形成成分によって囲まれた物質封入成分と、
iii.前記ナノ粒子組成物の内部に封入された金属体と、
を含むナノ粒子組成物を提供する。
(i)初速度:
a.ベシクル形成成分と、前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物を用意する工程と、
b.金属体を含む溶液内において前記ナノ粒子組成物を22℃よりも高い温度で培養することによって前記ナノ粒子組成物の内部に金属体を封入する工程と、
を含む。
a.ベシクル形成成分と、前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物を用意する工程と、
b.金属体を含む溶液内において前記ナノ粒子組成物を培養することにより、前記ベシクル形成成分の膜を透過するカチオン金属体の移動を可能とすることによって前記ナノ粒子組成物の内部に前記金属体を封入する工程と、
を含む。
a.i)ベシクル形成成分と、ii)前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物と、
b.前記ナノ粒子に封入される金属体を含む組成物と、
を含むことができる(各成分は本願明細書に記載するとおりである)。
本発明によれば、キット・オブ・パーツは、
a.i)ベシクル形成成分と、ii)前記ベシクル形成成分によって囲まれた物質封入成分と、iii)MRIに有用な金属体と、を含むナノ粒子組成物と、
b.前記ナノ粒子に封入される1種以上の金属体を含む組成物と、
を含む(各成分は本願明細書に記載するとおりである)か、
a.i)ベシクル形成成分と、ii)前記ベシクル形成成分によって囲まれた物質封入成分と、を含むナノ粒子組成物と、
b.前記ナノ粒子に封入される1種以上の金属体を含む組成物と、
を含む(各成分は本願明細書に記載するとおりである)ことができる。
a.ベシクル形成成分と、物質封入成分と、1種以上の封入金属体と、を含むナノ粒子組成物を用意することと、
b.前記ナノ粒子組成物を投与を必要とする対象者に投与することと、
を含む方法を提供する。
a.ベシクル形成成分と、物質封入成分と、ナノ粒子内に封入された1種以上の放射性核種と、を含むナノ粒子組成物を用意することと、
b.前記ナノ粒子組成物を対象者に静脈内投与することと、
c.所与の培養時間後にリポソーム組成物内における放射性核種から放射された放射線量を測定することと、
を含むか、
a.ベシクル形成成分と、物質封入成分と、ナノ粒子内に封入された1種以上の金属体と、を含むナノ粒子組成物を用意することと、
b.前記ナノ粒子組成物を対象者に静脈内投与することと、
c.従来の画像検査法を使用して前記対象者における前記金属体の存在及び/又は位置を測定することと、
を含む方法を提供する。
上述したように、等張HEPES緩衝液(10mM HEPES、150mM NaCl、pH7.4、300mOsm/L)を使用した場合には5.3%の放射線がリポソームに結合/封入されたが(表3)、一価イオン(Na+及びCl-)を添加しない場合には(10mM HEPES、pH7.4、5mOsm/L)、11%の放射線がDSPC/CHOL膜(50mM)に結合した(表5を参照)。
ただし、乾燥64CuCl2の溶解性は、pH7.4及び22℃の温度においてPBS及び滅菌水と比較してHEPES緩衝液においてより高いことが分かった。これは調製する際に都合が良い。より高い温度では、HEPES、PBS及び滅菌水内における乾燥64CuCl2の溶解性は同等だった。
(i)初速度:
Allen, et al. Biochim, Biophys. Acta, 597:418-426, 1980
Allen, Science, 303: 1818-1822, 2004
Altenbach and Seelig, Biochemistry, 23:3913-3920, 1984
Anderson et al., J Nucl Med., 36: 2315-2325, 1998
Binder et al., Bio-phys. Chem., 90:57-74, 2001
Binder and Zschornig, Chem. Phys. Lipids, 1 15:39-61 , 2002 Ceh et al., J. Phys. Chem. B, 102:3036-3043, 1998
Dehdashti et al., J Nucl Med. 38: 103P, 1997
Gabizon et al., J Liposome Res., 1 : 123-125, 1988
Gabizon et al., Cancer Res., 50: 6371-6378, 1990
Goto et al., Chem harm Bull. (Tokyo), 37: 1351-1354, 1989
Hauser and Dawson, J. Biochem., 1 :61-69, 1967
Hauser et al., Nature, 239:342-344, 1972
Henriksen et al., Nucl Med Bio., 31 : 441-449, 2004
Huster et al., Biophys. J., 78:3011-3018, 2000
Hwang et al., Biochim Biophys Acta., 716: 101-109, 1982
Kostarelos et al., J Liposome Res, 9:407-424, 1999
Lyklema, ISBN:0-12-460530-3, 5:3.208, 1995
Mash and Chin, Anal. Chem., 75:671-677, 2003
Mills et al., Biochim. Biophys. Acta, 1716:77-96, 2005
Morgan et al., J Med Microbiol., 14: 213-217, 1981
Papahadjopoulos et al., Biochim. Biophys. Acta, 266:561-583, 1971 Paula et al., Biophys. J., 74:319-327, 1998
Petersen et al., 2011 , Biomaterials, 32:2334-2341 , 201 1 Phillips, Adv Drug Deliv Rev., 37: 13-32, 1999
Phillips et al., Int J Rad AppI Instrum B, 19: 539-547, 1992 Puskin, J. Membrane Biol, 35:39-55, 1977
Seo et al., Bioconjucate Chem., 19: 2577-2584, 2008 Seo, Curr. Radiopharm., 1 : 17-21 , 2008
Sokolowska and Bal, J. Inorg. Biochem., 99: 1653-1660, 2005
Claims (40)
- 金属体が封入されたナノ粒子組成物の製造方法であって、
a.ベシクル形成成分と、前記ベシクル形成成分によって囲まれた水溶性及び非親油性キレート剤と、を含むナノ粒子組成物を用意することと、
b.カチオン金属体を含む溶液内において前記ナノ粒子組成物を培養することにより、前記ベシクル形成成分によって形成された膜を透過するカチオン金属体の移動を可能とすることによってイオノフォアを輸送分子として使用することなく前記ナノ粒子組成物の内部に前記金属体を封入する工程と、
を含む方法。 - 前記金属体が放射性核種である、請求項1に記載の方法。
- 放射性核種の封入効率が、10%よりも高い、請求項2に記載の方法。
- 前記ナノ粒子組成物を100℃未満の温度で培養する、請求項1〜3のいずれか一項に記載の方法。
- 前記ナノ粒子組成物を10〜80℃の温度で培養する、請求項1〜4のいずれか1項に記載の方法。
- 前記ナノ粒子組成物を48時間未満培養する、請求項1〜5のいずれか1項に記載の方法。
- 前記ナノ粒子組成物を1〜240分間培養する、請求項1〜6のいずれか1項に記載の方法。
- 前記ナノ粒子組成物を1〜120分間培養する、請求項1〜7のいずれか1項に記載の方法。
- 前記ナノ粒子組成物を1〜60分間培養する、請求項1〜8のいずれか1項に記載の方法。
- 培養時間が1〜240分間の場合の前記封入効率が10〜100%である、請求項1〜9のいずれか1項に記載の方法。
- 培養時間が1〜240分間の場合の前記封入効率が80〜100%である、請求項1〜10のいずれか1項に記載の方法。
- 培養時間が1〜240分間の場合の前記封入効率が95〜100%である、請求項1〜11のいずれか1項に記載の方法。
- ナノ粒子の内部に前記金属体を封入するための培養温度が30〜80℃であり、培養時間が1〜240分間の場合の前記封入効率が10〜100%である、請求項1〜12のいずれか1項に記載の方法。
- ナノ粒子の内部に前記金属体を封入するための培養温度が30〜80℃であり、培養時間が1〜60分間の場合の前記封入効率が10〜100%である、請求項1〜13のいずれか1項に記載の方法。
- ナノ粒子の内部に前記金属体を封入するための培養温度が30〜80℃であり、培養時間が1〜60分間の場合の前記封入効率が80〜100%である、請求項1〜14のいずれか1項に記載の方法。
- ナノ粒子の内部に前記金属体を封入するための培養温度が40〜80℃であり、培養時間が1〜60分間の場合の前記封入効率が95〜100%である、請求項1〜15のいずれか1項に記載の方法。
- 前記金属体はカチオンである、請求項1〜16のいずれか1項に記載の方法。
- 前記カチオン金属体は二価又は三価カチオンである、及び/又は前記金属体は二価又は三価カチオンである、請求項1〜17のいずれか1項に記載の方法。
- 前記金属体は、銅(61Cu、64Cu、67Cu)、インジウム(111In)、テクネチウム(99mTc)、レニウム(186Re、188Re)、ガリウム(67Ga、68Ga)、ストロンチウム(89Sr)、サマリウム(153Sm)、イッテルビウム(169Yb)、タリウム(201Tl)、アスタチン(211At)、ルテチウム(177Lu)、アクチニウム(225Ac)、イットリウム(90Y)、アンチモン(119Sb)、スズ(117Sn、113Sn)、ジスプロシウム(159Dy)、コバルト(56Co)、鉄(59Fe)、ルテニウム(97Ru、103Ru)、パラジウム(103Pd)、カドミウム(115Cd)、テルル(118Te、123Te)、バリウム(131Ba、140Ba)、ガドリニウム(149Gd、151Gd)、テルビウム(160Tb)、金(198Au、199Au)、ランタン(140La)及びラジウム(223Ra、224Ra)からなる群から選択される1種以上の放射性核種を含む、請求項1〜18のいずれか1項に記載の方法。
- 前記金属体は、61Cu、64Cu、67Cu、177Lu、67Ga、68Ga、225Ac、90Y、186Re、188Re、119Sb及び111Inからなる群から選択される放射性核種である、請求項1〜19のいずれか1項に記載の方法。
- 前記金属体は、61Cu、64Cu、67Cu、111In及び177Luからなる群から選択される放射性核種である、請求項1〜20のいずれか1項に記載の方法。
- 前記金属体は、61Cu、64Cu及び67Cuからなる群から選択される放射性核種である、請求項1〜21のいずれか1項に記載の方法。
- 1種以上の金属体が、Gd、Dy、Ti、Cr、Mn、Fe、Co、Ni及びそれらの二価又は三価イオンからなる群から選択される、請求項1〜22のいずれか1項に記載の方法。
- 前記金属体は、64Cu及びGd(III)、64Cu及びDy(III)、64Cu及びTi(II)、64Cu及びCr(III)、64Cu及びMn(II)、64Cu及びFe(II)、64Cu及びFe(III)、64Cu及びCo(II)、64Cu及びNi(II)、68Ga及びGd(III)、68Ga及びDy(III)、68Ga及びTi(II)、68Ga及びCr(III)、68Ga及びMn(II)、68Ga及びFe(II)、68Ga及びFe(III)、68Ga及びCo(II)、68Ga及びNi(II)、111In及びGd(III)、111In及びDy(III)、111In及びTi(II)、111In及びCr(III)、111In及びMn(II)、111In及びFe(II)、111In及びFe(III)、111In及びCo(II)、111In及びNi(II)、99mTc及びGd(III)、99mTc及びDy(III)、99mTc及びTi(II)、99mTc及びCr(III)、99mTc及びMn(II)、99mTc及びFe(II)、99mTc及びFe(III)、99mTc及びCo(II)、99mTc及びNi(II)、177Lu及びGd(III)、177Lu及びDy(III)、177Lu及びTi(II)、177Lu及びCr(III)、177Lu及びMn(II)、177Lu及びFe(II)、177Lu及びFe(III)、177Lu及びCo(II)、177Lu及びNi(II)、67Ga及びGd(III)、67Ga及びDy(III)、67Ga及びTi(II)、67Ga及びCr(III)、67Ga及びMn(II)、67Ga及びFe(II)、67Ga及びFe(III)、67Ga及びCo(II)、67Ga及びNi(II)、201Tl及びGd(III)、201Tl及びDy(III)、201Tl及びTi(II)、201Tl及びCr(III)、201Tl及びMn(II)、201Tl及びFe(II)、201Tl及びFe(III)、201Tl及びCo(II)、201Tl及びNi(II)、90Y及びGd(III)、90Y及びDy(III)、90Y及びTi(II)、90Y及びCr(III)、90Y及びMn(II)、90Y及びFe(II)、90Y及びFe(III)、90Y及びCo(II)、90Y及びNi(II)からなる群から選択される組み合わせであり、金属放射性核種の同位体は、一価カチオン、二価カチオン、三価カチオン、四価カチオン、五価カチオン、六価カチオン及び七価カチオンを含む金属の任意の酸化状態にある、請求項1〜23のいずれか1項に記載の方法。
- 前記金属体は、請求項19に記載の群から選択される2種以上の放射性核種である、請求項1〜24のいずれか1項に記載の方法。
- 前記金属体は、64Cu及び67Cu、61Cu及び67Cu、64Cu及び90Y、64Cu及び119Sb、64Cu及び225Ac、64Cu及び188Re、64Cu及び186Re、64Cu及び211At、64Cu及び67Ga、61Cu及び177Lu、61Cu及び90Y、61Cu及び119Sb、61Cu及び225Ac、61Cu及び188Re、61Cu及び186Re、61Cu及び211At、61Cu及び67Ga、67Cu及び177Lu、67Cu及び90Y、67Cu及び119Sb、67Cu及び225Ac、67Cu及び188Re、67Cu及び186Re、67Cu及び211At、68Ga及び177Lu、68Ga及び90Y、68Ga及び119Sb、68Ga及び225Ac、68Ga及び188Re、68Ga及び186Re、68Ga及び211At、68Ga及び67Cuからなる群から選択される2種類の放射性核種である、請求項1〜25のいずれか1項に記載の方法。
- 前記金属体は、銅(61Cu、64Cu及び67Cu)からなる群から選択される2種以上の放射性核種である、請求項1〜26のいずれか1項に記載の方法。
- 培養時にはナノ粒子の外部と前記ナノ粒子の内部との間に浸透圧差が存在する、請求項1〜27のいずれか1項に記載の方法。
- 前記ナノ粒子の外部と前記ナノ粒子の内部との間の浸透圧差は5〜800mOsm/Lである、請求項28に記載の方法。
- 前記ナノ粒子の外部と前記ナノ粒子の内部との間の浸透圧差は5〜100mOsm/Lである、請求項28又は29に記載の方法。
- 前記ベシクル形成成分は、脂質、セラミド、スフィンゴ脂質、リン脂質及びPEG化リン脂質からなる群から選択される1種以上の化合物を含む、請求項1〜30のいずれか1項に記載の方法。
- 前記ベシクル形成成分は、HSPC、DSPC、DPPC、POPC、CHOL、DSPE−PEG−2000及びDSPE−PEG−2000−TATEからなる群から選択される1種以上の両親媒性化合物を含む、請求項1〜31のいずれか1項に記載の方法。
- 前記キレート剤が、1,4,7,10−テトラアザシクロドデカン([12]aneN4)、1,4,7,10−テトラアザシクロトリデカン([13]aneN4)、1,4,8,11−テトラアザシクロテトラデカン([14]aneN4)、1,4,8,12−テトラアザシクロペンタデカン([15]aneN4)、1,5,9,13−テトラアザシクロヘキサデカン([16]aneN4)、エチレンジアミン四酢酸(EDTA)及びジエチレントリアミン五酢酸(DTPA)からなる群から選択される、請求項1〜32のいずれか1項に記載の方法。
- 前記キレート剤が、1,4−エタノ−1,4,8,11−テトラアザシクロテトラデカン(et−シクラム)、1,4,7,11−テトラアザシクロテトラデカン(iso−シクラム)、1,4,7,10−テトラアザシクロドデカン−1,4,7,10−四酢酸(DOTA)、2−(1,4,7,10−テトラアザシクロドデカン−1−イル)酢酸(DO1A)、2,2’−(1,4,7,10−テトラアザシクロドデカン−1,7−ジイル)二酢酸(DO2A)、2,2’,2’’−(1,4,7,10−テトラアザシクロドデカン−1,4,7−トリイル)三酢酸(DO3A)、1,4,7,10−テトラアザシクロドデカン−1,4,7,10−テトラ(メタンホスホン酸)(DOTP)、1,4,7,10−テトラアザシクロドデカン−1,7−ジ(メタンホスホン酸)(DO2P)、1,4,7,10−テトラアザシクロドデカン−1,4,7−トリ(メタンホスホン酸)(DO3P)、1,4,8,11−15テトラアザシクロテトラデカン−1,4,8,11−四酢酸(TETA)、2−(1,4,8,11−テトラアザシクロテトラデカン−1−イル)酢酸(TE1A)、2,2’−(1,4,8,11−テトラアザシクロテトラデカン−1,8−ジイル)二酢酸(TE2A)、エチレンジアミン四酢酸(EDTA)及びジエチレントリアミン五酢酸(DTPA)からなる群から選択される、請求項1〜33のいずれか1項に記載の方法。
- 前記キレート剤が、1,4,7,10−テトラアザシクロドデカン−1,4,7,10−四酢酸(DOTA)、1,4,8,11−15テトラアザシクロテトラデカン−1,4,8,11−四酢酸(TETA)、1,4,7,10−テトラアザシクロドデカン−1,4,7,10−テトラ(メタンホスホン酸)(DOTP)、シクラム及びシクレンからなる群から選択される、請求項1〜34のいずれか1項に記載の方法。
- 前記ナノ粒子の内部pHは、4〜8.5である、請求項1〜35のいずれか1項に記載の方法。
- 前記放射性標識ナノ粒子は、20%未満の放射線の漏出が観察される安定性を有する、請求項1〜36のいずれか1項に記載の方法。
- イオノフォアを輸送分子として使用せずにナノ粒子内へ金属体の封入を行うためのキット・オブ・パーツであって、
a.i)ベシクル形成成分と、ii)前記ベシクル形成成分によって囲まれた水溶性及び非親油性キレート剤と、を含むナノ粒子組成物と、
b.前記ナノ粒子に封入されるカチオン金属体を含む組成物とを含み、
c.前記キットはイオノフォアを含まない、
キット・オブ・パーツ。 - 前記金属体は、請求項17〜27のいずれか1項に記載の放射性核種の1種以上を含む、請求項38に記載のキット・オブ・パーツ。
- 前記金属体は銅同位体(61Cu、64Cu及び67Cu)から選択される1種以上の放射性核種である、請求項38又は39に記載のキット・オブ・パーツ。
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DKPA201070542 | 2010-12-14 | ||
DKPA201070542 | 2010-12-14 | ||
US201161434070P | 2011-01-19 | 2011-01-19 | |
EP11151372.7 | 2011-01-19 | ||
US61/434,070 | 2011-01-19 | ||
EP11151372 | 2011-01-19 | ||
PCT/DK2011/050479 WO2012079582A1 (en) | 2010-12-14 | 2011-12-14 | Entrapment of radionuclides in nanoparticle compositions |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2014506240A JP2014506240A (ja) | 2014-03-13 |
JP2014506240A5 JP2014506240A5 (ja) | 2015-02-05 |
JP5947807B2 true JP5947807B2 (ja) | 2016-07-06 |
Family
ID=45445682
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013543530A Expired - Fee Related JP5947807B2 (ja) | 2010-12-14 | 2011-12-14 | ナノ粒子組成物への放射性核種の封入 |
Country Status (10)
Country | Link |
---|---|
US (2) | US9226984B2 (ja) |
EP (1) | EP2651447B1 (ja) |
JP (1) | JP5947807B2 (ja) |
KR (1) | KR20140092226A (ja) |
AU (1) | AU2011344865B2 (ja) |
BR (1) | BR112013014735A2 (ja) |
CA (1) | CA2821024A1 (ja) |
DK (1) | DK2651447T3 (ja) |
RU (1) | RU2013132610A (ja) |
WO (1) | WO2012079582A1 (ja) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2881928A1 (en) | 2012-04-17 | 2013-10-24 | Merrimack Pharmaceuticals, Inc. | Compositions and methods for non-invasive imaging |
US9717724B2 (en) | 2012-06-13 | 2017-08-01 | Ipsen Biopharm Ltd. | Methods for treating pancreatic cancer using combination therapies |
AU2013202947B2 (en) | 2012-06-13 | 2016-06-02 | Ipsen Biopharm Ltd. | Methods for treating pancreatic cancer using combination therapies comprising liposomal irinotecan |
US9993427B2 (en) * | 2013-03-14 | 2018-06-12 | Biorest Ltd. | Liposome formulation and manufacture |
US20160303264A1 (en) * | 2013-10-23 | 2016-10-20 | Merrimack Pharmaceuticals, Inc. | Liposomes useful for non-invasive imaging and drug delivery |
TW201615229A (zh) * | 2014-10-23 | 2016-05-01 | 行政院原子能委員會核能研究所 | 製備放射標靶藥物的套件及放射標靶藥物之製造方法 |
AU2016256979B2 (en) | 2015-05-04 | 2021-01-28 | Versantis AG | Method for preparing transmembrane pH-gradient vesicles |
US11318131B2 (en) | 2015-05-18 | 2022-05-03 | Ipsen Biopharm Ltd. | Nanoliposomal irinotecan for use in treating small cell lung cancer |
AU2016309002B2 (en) | 2015-08-20 | 2021-07-29 | Ipsen Biopharm Ltd. | Combination therapy using liposomal irinotecan and a PARP inhibitor for cancer treatment |
JP2018528185A (ja) | 2015-08-21 | 2018-09-27 | イプセン バイオファーム リミティド | リポソーム型イリノテカン及びオキサリプラチンを含む組み合わせ療法を使用して転移性膵臓癌を治療するための方法 |
RU2599462C1 (ru) * | 2015-09-22 | 2016-10-10 | Общество с ограниченной ответственностью "БИОТЕХНОЛОГИЯ" (ООО "БИОТЕХНОЛОГИЯ") | Способ полисигнальной активации апоптоза клеток злокачественных солидных опухолей |
KR20180063255A (ko) | 2015-10-16 | 2018-06-11 | 입센 바이오팜 리미티드 | 캄프토테신 제약 조성물의 안정화 |
EP3354270A4 (en) * | 2016-10-21 | 2019-04-24 | Obshestvo S Ogranichennoi Otvetstvennost'yu "Biotehnologiya" | METHOD FOR ACTIVATION OF APOPTOSIS OF CELLS WITH MULTIPLE SIGNALING OF SOLID MALIGNANT TUMORS |
CA3040395A1 (en) | 2016-11-02 | 2018-05-11 | Ipsen Biopharm Ltd. | Treating gastric cancer using combination therapies comprising liposomal irinotecan, oxaliplatin, 5-fluoruracil (and leucovorin) |
US11798700B2 (en) | 2018-03-26 | 2023-10-24 | The University Of British Columbia | Systems, apparatus and methods for separating actinium, radium, and thorium |
CN109063231B (zh) * | 2018-06-15 | 2023-06-27 | 中国核电工程有限公司 | 基于GUM导则的核素不确定度对临界系统keff影响的评定方法 |
US11471497B1 (en) | 2019-03-13 | 2022-10-18 | David Gordon Bermudes | Copper chelation therapeutics |
WO2023183559A1 (en) * | 2022-03-24 | 2023-09-28 | The Brigham And Women's Hospital, Inc. | Engineered ionophores for transport of metal ions |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4310506A (en) * | 1979-02-22 | 1982-01-12 | California Institute Of Technology | Means of preparation and applications of liposomes containing high concentrations of entrapped ionic species |
US5077056A (en) | 1984-08-08 | 1991-12-31 | The Liposome Company, Inc. | Encapsulation of antineoplastic agents in liposomes |
US5736155A (en) | 1984-08-08 | 1998-04-07 | The Liposome Company, Inc. | Encapsulation of antineoplastic agents in liposomes |
US4753788A (en) * | 1985-01-31 | 1988-06-28 | Vestar Research Inc. | Method for preparing small vesicles using microemulsification |
US5622713A (en) | 1985-09-17 | 1997-04-22 | The Regents Of The University Of California | Method of detoxifying animal suffering from overdose |
CA1314209C (en) | 1987-11-04 | 1993-03-09 | Gary Fujii | Composition and method for use for liposome encapsulated compounds for neutron capture tumor therapy |
US5258499A (en) | 1988-05-16 | 1993-11-02 | Vestar, Inc. | Liposome targeting using receptor specific ligands |
US5688488A (en) | 1989-04-03 | 1997-11-18 | Purdue Research Foundation | Composition and method for tumor imaging |
US5013556A (en) | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
US5525232A (en) | 1990-03-02 | 1996-06-11 | The Liposome Company, Inc. | Method for entrapment of cationic species in lemellar vesicles |
JPH075561B2 (ja) | 1991-12-17 | 1995-01-25 | 工業技術院長 | α−アミノ酸のジアミド誘導体 |
CA2093381A1 (en) * | 1992-04-07 | 1993-10-08 | Hideyuki Sawahara | Liposome formulation and process for production thereof |
US5837282A (en) * | 1996-10-30 | 1998-11-17 | University Of British Columbia | Ionophore-mediated liposome loading |
US6306393B1 (en) * | 1997-03-24 | 2001-10-23 | Immunomedics, Inc. | Immunotherapy of B-cell malignancies using anti-CD22 antibodies |
US6106858A (en) * | 1997-09-08 | 2000-08-22 | Skyepharma, Inc. | Modulation of drug loading in multivescular liposomes |
US5945502A (en) | 1997-11-13 | 1999-08-31 | Xerox Corporation | Electroluminescent polymer compositions and processes thereof |
NO312708B1 (no) * | 2000-02-21 | 2002-06-24 | Anticancer Therapeutic Inv Sa | Radioaktive liposomer til terapi |
EP1420831A1 (en) * | 2001-07-27 | 2004-05-26 | Targesome, Inc. | Lipid constructs as therapeutic and imaging agents |
ES2290333T3 (es) | 2001-11-13 | 2008-02-16 | Celator Pharmaceuticals, Inc. | Composiciones de vehiculos lipidicos y metodos para la retencion mejorada de farmacos. |
TW200303216A (en) * | 2002-02-26 | 2003-09-01 | Amato Pharm Prod Ltd | Method of encapsulating metal complex within liposomes |
EP1616182A4 (en) | 2003-03-18 | 2008-04-16 | Ethicon Inc | REPLACEMENT ENZYMOTHERAPY WITH 17-BETA-HYDROXYSTEROID DESHYDROGENASE TYPE 2 |
EP1603535A4 (en) | 2003-03-18 | 2008-10-15 | Ethicon Inc | AROMATASE HEMMER DIAGNOSIS AND THERAPY |
JP2006045132A (ja) * | 2004-08-05 | 2006-02-16 | Konica Minolta Medical & Graphic Inc | リポソーム含有磁気共鳴造影剤 |
US20060040980A1 (en) | 2004-08-20 | 2006-02-23 | Lind Stuart E | Ionophores as cancer chemotherapeutic agents |
GB0423565D0 (en) | 2004-10-22 | 2004-11-24 | Algeta As | Formulation |
ITMI20050328A1 (it) | 2005-03-03 | 2006-09-04 | Univ Degli Studi Milano | Composti peptidomimetrici e preparazione di derivati biologicamente attivi |
TW200922630A (en) | 2007-09-26 | 2009-06-01 | Nat Health Research Institutes | Liposome compositions useful for tumor imaging and treatment |
WO2009140215A2 (en) | 2008-05-11 | 2009-11-19 | Geraghty, Erin | Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds |
JP5429710B2 (ja) * | 2009-03-30 | 2014-02-26 | 独立行政法人放射線医学総合研究所 | 治療薬剤の標的部位への集積及び放出を追跡可能な治療薬剤含有リポソームおよびその製造方法 |
US8920775B2 (en) | 2009-07-17 | 2014-12-30 | Technical University Of Denmark | Loading technique for preparing radionuclide containing nanoparticles |
-
2011
- 2011-12-14 WO PCT/DK2011/050479 patent/WO2012079582A1/en active Application Filing
- 2011-12-14 RU RU2013132610/15A patent/RU2013132610A/ru not_active Application Discontinuation
- 2011-12-14 BR BR112013014735A patent/BR112013014735A2/pt not_active IP Right Cessation
- 2011-12-14 KR KR1020137017922A patent/KR20140092226A/ko not_active Application Discontinuation
- 2011-12-14 US US13/992,080 patent/US9226984B2/en not_active Expired - Fee Related
- 2011-12-14 JP JP2013543530A patent/JP5947807B2/ja not_active Expired - Fee Related
- 2011-12-14 CA CA2821024A patent/CA2821024A1/en not_active Abandoned
- 2011-12-14 EP EP11804942.8A patent/EP2651447B1/en not_active Not-in-force
- 2011-12-14 AU AU2011344865A patent/AU2011344865B2/en not_active Ceased
- 2011-12-14 DK DK11804942.8T patent/DK2651447T3/en active
-
2015
- 2015-12-14 US US14/968,019 patent/US20160158392A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
WO2012079582A1 (en) | 2012-06-21 |
JP2014506240A (ja) | 2014-03-13 |
DK2651447T3 (en) | 2018-12-17 |
KR20140092226A (ko) | 2014-07-23 |
BR112013014735A2 (pt) | 2016-10-04 |
RU2013132610A (ru) | 2015-01-20 |
EP2651447A1 (en) | 2013-10-23 |
CA2821024A1 (en) | 2012-06-21 |
US20160158392A1 (en) | 2016-06-09 |
US9226984B2 (en) | 2016-01-05 |
AU2011344865A1 (en) | 2013-07-11 |
US20130251630A1 (en) | 2013-09-26 |
AU2011344865B2 (en) | 2017-03-09 |
EP2651447B1 (en) | 2018-08-29 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5947807B2 (ja) | ナノ粒子組成物への放射性核種の封入 | |
JP5872466B2 (ja) | 放射性核種含有ナノ粒子を製造するための封入方法 | |
Soundararajan et al. | [186Re] Liposomal doxorubicin (Doxil): in vitro stability, pharmacokinetics, imaging and biodistribution in a head and neck squamous cell carcinoma xenograft model | |
Petersen et al. | 64Cu loaded liposomes as positron emission tomography imaging agents | |
Boerman et al. | Radiolabeled liposomes for scintigraphic imaging | |
Henriksen et al. | Remote loading of 64Cu2+ into liposomes without the use of ion transport enhancers | |
KR20140097215A (ko) | 암 치료를 위한 조합 리포좀 조성물 | |
Cvjetinović et al. | Bioevaluation of glucose-modified liposomes as a potential drug delivery system for cancer treatment using 177-Lu radiotracking | |
Engudar et al. | Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model | |
Kaul et al. | Targeted theranostic liposomes: rifampicin and ofloxacin loaded pegylated liposomes for theranostic application in mycobacterial infections | |
Van Der Geest et al. | Comparison of three remote radiolabelling methods for long-circulating liposomes | |
Isaac-Olivé et al. | [99m Tc-HYNIC-N-dodecylamide]: a new hydrophobic tracer for labelling reconstituted high-density lipoproteins (rHDL) for radioimaging | |
Fragogeorgi et al. | Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO) 3 labeled liposome | |
US20160038597A9 (en) | Carrier that targets fucosylated molecule-producing cells | |
WO2023014975A1 (en) | Methods for biological material labeling and medical imaging | |
Wallingford et al. | Is stability a key parameter in the accumulation of phospholipid vesicles in tumors? | |
Laverman et al. | Radiolabeling of liposomes for scintigraphic imaging | |
US20240148918A1 (en) | Loading of Alginate Microspheres | |
Gregory | Radiolabeling of Liposomes for Scintigraphic Imaging | |
Prasad | ALPHA-PARTICLE NANOTHERAPEUTICS AGAINST METASTATIC AND/OR CHEMORESISTANT TRIPLE NEGATIVE BREAST CANCER | |
Amanlou et al. | Magnetic resonance contrast media sensing in vivo molecular imaging agents: an overview | |
CA3212641A1 (en) | Loading of alginate microspheres | |
Mishra | Exploring pretargeted PET imaging strategies for liposomal nanomedicines | |
CN116143826A (zh) | 一种有助于诊疗的新型硼脂质体 | |
Locke | STRATEGIES FOR TARGETED IMAGING OF LEUKOCYTES IN THE LUNG |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A521 | Written amendment |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20141204 |
|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20141204 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20151014 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20151224 |
|
A521 | Written amendment |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160114 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20160511 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20160603 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 5947807 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
LAPS | Cancellation because of no payment of annual fees |