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Substance-containing vesicle, and production method therefor

外国特許コード F170009180
整理番号 AF12-14WO
掲載日 2017年9月12日
出願国 アメリカ合衆国
出願番号 201514839854
公報番号 20160051484
公報番号 9782358
出願日 平成27年8月28日(2015.8.28)
公報発行日 平成28年2月25日(2016.2.25)
公報発行日 平成29年10月10日(2017.10.10)
優先権データ
  • 特願2013-041186 (2013.3.1) JP
  • 特願2013-176068 (2013.8.27) JP
  • 2014WO-JP55186 (2014.2.28) WO
発明の名称 (英語) Substance-containing vesicle, and production method therefor
発明の概要(英語) (US9782358)
Provided is a monodisperse agglomerate of a substance-containing vesicle filled with a substance at a concentration higher than conventionally possible.
A mixed solution, in which a target substance is included in an aqueous medium, is mixed with a monodisperse agglomerate of a crosslinked vesicle comprising a prescribed polymer which includes a first polymer, i.e. a block copolymer having uncharged hydrophilic segments and first charged segments, and a second polymer having second charged segments carrying a charge opposite to that of the first charged segments, and in which the first polymer and/or the second polymer are/is crosslinked.
As a result, the crosslinked vesicle is made to contain the target substance.
特許請求の範囲(英語) [claim1]
1. A monodisperse population of substance-encapsulating crosslinked vesicles, each of the substance-encapsulating crosslinked vesicles comprising: a crosslinked membrane comprising a first polymer, which is block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment, the first and/or the second polymer(s) being crosslinked;
an inner aqueous phase surrounded by the crosslinked membrane; and
a target substance encapsulated in the inner aqueous phase,
wherein the concentration of the target substance encapsulated in the inner aqueous phase is higher than 5mg/mL.
[claim2]
2. The monodisperse population of substance-encapsulating crosslinked vesicles according to claim 1, having a polydispersity index of 0.2 or lower.
[claim3]
3. The monodisperse population of substance-encapsulating crosslinked vesicles according to claim 1 or 2, wherein the weight-average molecular weight of the target substance is between 10000 and 40000.
[claim4]
4. The monodisperse population of substance-encapsulating crosslinked vesicles according to claim 2, wherein the first and/or the second polymer(s) is(are) crosslinked with one or more crosslinking bonds selected from the group consisting of a crosslinking bond formed between cationic groups, a crosslinking bond formed between anionic groups, and a crosslinking bond formed between a cationic group and an anionic group, and the molar ratio of the cationic groups and/or anionic groups forming crosslinking bonds to the cationic groups and/or anionic groups contained in the crosslinked membrane is 35% or more.
[claim5]
5. A substance-encapsulating crosslinked vesicles comprising: a crosslinked membrane comprising a first polymer, which is block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment, the first and/or the second polymer(s) being crosslinked;
an inner aqueous phase surrounded by the crosslinked membrane; and
a first target substance and a second target substance encapsulated in the inner aqueous phase, wherein the first target substance having a smaller molecular weight than the molecular weight of the second target substance, and the second target substance is a crowding agent,
wherein the first target substance is more stable than when the first target substance is contained in the inner aqueous phase in the absence of the second target substance.
[claim6]
6. A method of producing a substance-encapsulating vesicle, comprising mixing a monodisperse population of vacant crosslinked vesicles with a mixture liquid containing the target substance in an aqueous medium to form a monodisperse population of substance-encapsulating crosslinked vesicles, wherein each of the vacant crosslinked vesicles comprises: a crosslinked membrane comprising a first polymer, which is block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment, the first and/or the second polymer(s) being crosslinked; and an inner aqueous phase surrounded by the crosslinked membrane, wherein the inner aqueous phase does not contain the target substance, and
wherein each of the substance-encapsulating crosslinked vesicles comprises: the crosslinked membrane comprising the first polymer and the second polymer, the first and/or the second polymer(s) being crosslinked; and the inner aqueous phase surrounded by the crosslinked membrane, wherein the inner aqueous phase contains the target substance.
[claim7]
7. The method according to claim 6, wherein the monodisperse population of vacant crosslinked vesicles, the monodisperse population of substance-encapsulating crosslinked vesicles, the monodisperse population of vacant non-crosslinked vesicles, and the monodisperse population of substance-encapsulating non-crosslinked vesicles each have a polydispersity index of 0.2 or less.
[claim8]
8. The method according to claim 6 or 7, wherein the weight-average molecular weight of the target substance is between 10000 and 40000, and the concentration of the target substance in the mixture liquid is more than 5 mg/mL.
[claim9]
9. The method according to claim 8, wherein both in the vacant crosslinked vesicles and the substance-encapsulating crosslinked vesicles, the first and/or the second polymer(s) is(are) crosslinked with one or more crosslinking bonds selected from the group consisting of a crosslinking bond formed between cationic groups, a crosslinking bond formed between anionic groups, and a crosslinking bond formed between a cationic group and an anionic group, and the molar ratio of the cationic groups and/or anionic groups forming crosslinking bonds to the cationic groups and/or anionic groups contained in the crosslinked membrane is 35% or more.
[claim10]
10. The method according to claim 6, further comprising: reacting the monodisperse population of substance-encapsulating crosslinked vesicles with a crosslinker which can react with the first and/or the second polymer(s).
[claim11]
11. A method of producing a substance-encapsulating vesicle, comprising: mixing a first substance-encapsulating crosslinked vesicle, which encapsulates a first target substance, with a mixture liquid containing a second target substance in an aqueous medium to form a second substance-encapsulating crosslinked vesicle,
wherein the first substance-encapsulating crosslinked vesicle comprises: a crosslinked membrane comprising a first polymer, which is block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment, the first and/or the second polymer(s) being crosslinked; and an inner aqueous phase surrounded by the crosslinked membrane, wherein the inner aqueous phase contains the first target substance, and
wherein the second substance-encapsulating crosslinked vesicle comprises: the crosslinked membrane comprising the first polymer and the second polymer, the first and/or the second polymer(s) being crosslinked; and the inner aqueous phase surrounded by the crosslinked membrane, wherein the inner aqueous phase contains the first target substance and the second target substances.
[claim12]
12. The method according to claim 11, wherein a monodisperse population of the first substance-encapsulating crosslinked vesicles is used to thereby produce a monodisperse population of the second substance-encapsulating crosslinked vesicles.
[claim13]
13. The method according to claim 12, wherein the concentration of the second target substance contained in the mixture liquid is high enough to prevent formation of a monodisperse population of substance-encapsulating non-crosslinked vesicles each encapsulating both the first and second target substances when a monodisperse population of first non-crosslinked vesicles is mixed with the mixture liquid, wherein the monodisperse population of first substance-encapsulating non-crosslinked vesicles differs from the monodisperse population of first substance-encapsulating crosslinked vesicles only in that the first and/or the second polymer(s) is(are) not crosslinked.
[claim14]
14. The method according to any one of claims 11 to 13, further comprising forming the first substance-encapsulating crosslinked vesicle by contacting a vacant crosslinked vesicle a mixture liquid containing the first target substance in an aqueous medium, wherein the vacant crosslinked vesicle comprises a crosslinked membrane comprising: the first and second polymers wherein the first and/or the second polymer(s) is(are) crosslinked; and an inner aqueous phase surrounded by the crosslinked membrane, wherein the inner aqueous phase does not contain the first and second target substances; and
if necessary, reacting the vesicle with a crosslinker which can react with the first and/or the second polymer(s).
[claim15]
15. The method according to claim 14, wherein a monodisperse population of the vacant crosslinked vesicles is used to thereby produce a monodisperse population of the first substance-encapsulating crosslinked vesicles.
[claim16]
16. The method according to claim 15, wherein the concentration of the first target substance contained in the mixture liquid is high enough to inhibit the formation of a monodisperse population of substance-encapsulating non-crosslinked vesicles containing the first target substance when a monodisperse population of vacant non-crosslinked vesicles is mixed with the mixture liquid, wherein the monodisperse population of vacant non-crosslinked vesicles differs from the monodisperse population of vacant crosslinked vesicles only in that the first and/or the second polymer(s) are not crosslinked.
[claim17]
17. The method according to claim 11, wherein the second target substance is a crowding agent.
[claim18]
18. A drug delivery system comprising the monodisperse population of vesicles according to claim 1.
[claim19]
19. A drug delivery system comprising the vesicles according to claim 5.
  • 発明者/出願人(英語)
  • KATAOKA KAZUNORI
  • KISHIMURA AKIHIRO
  • ANRAKU YASUTAKA
  • GOTO AKINORI
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
参考情報 (研究プロジェクト等) CREST Establishment of Innovative Manufacturing Technology Based on Nanoscience AREA
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