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Substance-containing vesicle, and production method therefor

外国特許コード F170009171
整理番号 AF12-14WO
掲載日 2017年9月12日
出願国 中華人民共和国
出願番号 201480012267
公報番号 105188905
出願日 平成26年2月28日(2014.2.28)
公報発行日 平成27年12月23日(2015.12.23)
国際出願番号 JP2014055186
国際公開番号 WO2014133172
国際出願日 平成26年2月28日(2014.2.28)
国際公開日 平成26年9月4日(2014.9.4)
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) (CN105188905)
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. Cross-linked mono-dispersion of microcapsules encapsulating a substance, characterized in,
And the cross-linked film comprising cross-linked film encloses an inner aqueous phase and in the internal aqueous phase into encapsulating the mono-dispersion of microcapsules encapsulating cross-linked material of a target substance,
Wherein the cross-linked film includes 1st charged with uncharged hydrophilic block and as a block copolymer of polymer block 1st, and has a band with the 1st 2nd charged blocks oppositely charged charged blocks of a polymer 2nd, 1st and the 2nd/or polymer and is cross-linked;
At a concentration of a target substance contained in the internal aqueous phase,
1st and the 2nd and/or non-cross linked polymer in the target substance under a non-encapsulated, mono-dispersion of microcapsules encapsulating cross-linked with the substance different empty Non-crosslinked microcapsules single-dispersion, mixing with the substance encapsulated cross-linked microcapsules containing the same concentration of inland waters of the target substance, and the case of a mixture of an aqueous medium,
A substance encapsulation Non-crosslinked microcapsules encapsulating the objective substance hindering the formation of a mono-dispersion of a concentration of.
[claim2]
2. In the mono-dispersion of microcapsules encapsulating cross-linked substance according to claim 1, characterized in, which has a polydispersity index of 0.2 or less.
[claim3]
3. According to claim 1 or 2 mono-dispersion of microcapsules encapsulating material in the cross-linked, characterized in, weight average molecular weight of 10000-40000 of a target substance, contained in the internal aqueous phase of a target substance concentration is more than 5 mg/mL.
[claim4]
4. In the mono-dispersion of microcapsules encapsulating cross-linked substance according to claim 3, characterized in, 1st and a 2nd/or polymer, by cross-linking bonds formed between the cationic groups are selected from, cross-linking bonds formed between anionic groups, cationic groups and cationic groups and the group consisting of cross-linking bonds formed between 1 kind or 2 kinds or more of a cross-linked by cross-linking bonds, a ratio of cross-linked film forming polymer capable of cationic groups and/or anionic groups contained in the total moles of 35% or more to.
[claim5]
5. A substance encapsulation Crosslinked microcapsules, characterized in,
And the cross-linked film comprising cross-linked film encloses an inner aqueous phase and in the internal aqueous phase into the target material and encapsulating the 1st 2nd 1st target substance than a substance having small molecular weight target substance encapsulated Crosslinked microcapsules,
1st target substance, as compared to the 2nd target substance is absent and contained in the aqueous phase is stable within a case;
Wherein the cross-linked film having uncharged hydrophilic block and comprising as 1st charged blocks of a block copolymer polymer 1st, 1st charged blocks and has oppositely charged 2nd band and the charged polymer block has a 2nd, 1st and the 2nd/or crosslinking of a polymer and made into.
[claim6]
6. According to claim 5 of a substance in Crosslinked microcapsules encapsulating, characterized in, 2nd target substance is a crowding agent.
[claim7]
7. A substance encapsulation process for the preparation of microcapsules, characterized in,
A mono-dispersion of microcapsules comprising an empty cross-linking, containing the target substance in the mixture, and a mixture of an aqueous medium, a mono-dispersion of microcapsules encapsulating cross-linking process of clutch means; mono-dispersion of microcapsules containing cross-linked its hollow cross-linked membrane enclosed into an inner aqueous phase and a cross-linked film, and in the internal aqueous phase a target substance is not encapsulated; comprising cross-linked film as having uncharged hydrophilic block and a block copolymer of polymer block charged 1st 1st, having a belt with the 1st and 2nd charged blocks oppositely charged charged blocks of a polymer 2nd, 1st and the 2nd/or polymer and is cross-linked;
In which the substance encapsulated 1st and the 2nd comprising a mono-dispersion of microcapsules containing cross-linked polymer by the 1st and the 2nd/or polymer and is cross-linked by cross-linked film, and the cross-linked film enclosed into an inner aqueous phase, and the target material encapsulating the internal aqueous phase.
[claim8]
8. In the method according to claim 7, characterized in, cross-linked microcapsules with a mono-dispersion empty, mono-dispersion of microcapsules encapsulating cross-linking agents, mono-dispersion of an empty Non-crosslinked microcapsules, and a mono-dispersion not more than 0.2 Non-crosslinked microcapsules encapsulating material has a polydispersity index of that.
[claim9]
9. In accordance with a method described in claim 7 or 8, characterized in, weight average molecular weight of 10000-40000 of a target substance, a mixture containing a target substance in a concentration of more than 5 mg/mL.
[claim10]
10. In the method according to claim 9, characterized in, empty cross-linked microcapsules and microcapsules encapsulating material, 1st and the 2nd polymer/or, by cross-linking bonds are formed between selected from the cationic groups, anionic groups to form crosslinks between, and cationic groups and cationic groups to form crosslinks between 1 or 2 group consisting of more than one cross-linking bonds in a cross-linked, in a proportion of cross-linking bonds formed, cationic groups and/or cross-linked film contains anionic groups to total number of moles of not less than 35%.
[claim11]
11. In accordance with the method according to any one of claim 7-10, characterized in, this method further comprises causing substance encapsulated cross-linked microcapsules with a 1st/2nd with a mono-dispersion and which can be obtained by reacting a polymer or cross-linking agent and a process of reacting is carried out.
[claim12]
12. A substance encapsulation process for the preparation of microcapsules, characterized in,
Which comprises the 1st Crosslinked microcapsules containing encapsulated material, mixed in 1st 2nd having small molecular weight than the target substance containing the target substance, and a mixture of an aqueous medium, and form a 2nd substance encapsulated cross-linked microcapsules with a process;
Wherein the 1st substance encapsulated cross-linked microcapsules containing cross-linked film, and the cross-linked film enclosed into an inner aqueous phase, and the target substance encapsulating the 1st internal aqueous phase, cross-linked film having uncharged hydrophilic block and comprising as 1st charged blocks of a block copolymer polymer 1st, 1st charged blocks and has oppositely charged 2nd band and the charged polymer block has a 2nd, 1st and the 2nd/or polymer and the cross-linked;
2nd 1st 2nd substance encapsulated Crosslinked microcapsules which contains a 1st and a 2nd/or and made of polymer and the polymer cross-linked by cross-linked film, and surrounded by the cross-linked film into an inner aqueous phase, 1st and the 2nd target substance is entrapped in the internal aqueous phase.
[claim13]
13. In the method according to claim 12, characterized in, cross-linked substance encapsulated microcapsule is a mono-dispersion 1st, 2nd substance encapsulated cross-linked microcapsules is a mono-dispersion.
[claim14]
14. In the method according to claim 13, characterized in, 2nd target specie concentration is contained in the mixture,
In a 1st and a 2nd/or in the case of non-cross linked polymer, cross-linked substance encapsulated mono-dispersion of microcapsules with the 1st 1st Non-crosslinked microcapsules encapsulating material different from that of a single-dispersion, in a case where mixed in the liquid mixture,
1st and 2nd Non-crosslinked microcapsules encapsulating material encapsulating the blocking target substance concentration formed of a single-dispersion.
[claim15]
15. Method according to any one of claim 12-14, characterized in,
The method further includes placing an empty Crosslinked microcapsules, containing 1st target substance mixed therewith, and a mixture of an aqueous medium, if necessary, 1st and the 2nd/or can be allowed to react with a crosslinking agent reactive polymer and the reaction, the process of forming 1st substance encapsulated cross-linked microcapsules;
Wherein the empty cross-linked microcapsule contains cross-linked film, and the cross-linked film enclosed into an inner aqueous phase, in the 1st and the 2nd internal aqueous phase with a non-encapsulated according to any one of a target substance;
Wherein the 1st and the 2nd polymer containing cross-linked film, 1st and the 2nd/or by cross-linked polymer.
[claim16]
16. In the method according to claim 15, characterized in, resembling a monomolecular dispersion thereof having a cross-linked microcapsule is empty, 1st substance encapsulated mono-dispersion of microcapsule is a cross-linked.
[claim17]
17. In the method according to claim 16, characterized in, 1st at a concentration of a target substance contained in the mixture,
1st/2nd or not cross-linked polymer in the case with, mono-dispersion of microcapsules encapsulating cross-linked with the empty Non-crosslinked microcapsules mixed mono-dispersion different empty encapsulated in the liquid mixture in the case of which,
1st Non-crosslinked microcapsules encapsulating material encapsulating the inhibit target substance concentration formed of a single-dispersion.
[claim18]
18. Method according to any one of claim 12-17, characterized in, 2nd target substance is a crowding agent.
[claim19]
19. An adsorbent material encapsulated microcapsules, characterized in,
As a non-charged hydrophilic block comprising a block comprising a block polymer of 1st and 1st charged polymer, and, has a 1st 2nd charged oppositely charged charged blocks 2nd polymer block formed of a film of a microcapsule, and the microcapsule-encapsulated adsorbent material particles, at least one of 1st and 2nd polymer adsorbed on the adsorbent material particles.
[claim20]
20. Encapsulated adsorbent material in the microcapsule according to claim 19, characterized in, 1st and the 2nd/or polymers are cross linked.
[claim21]
21. In accordance with an adsorbent material encapsulated in the microcapsules claim 19 or 20, characterized in, adsorbent material particles are silica particles.
[claim22]
22. In accordance with claim 19-21 encapsulated adsorbent material in any one microcapsule, characterized in, adsorbent material particles have an average particle diameter of 40 nm -10 μm.
[claim23]
23. Claim 19-22 encapsulated adsorbent material in the microcapsule according to any one, characterized in, on the adsorbent material particles to surface treatment.
[claim24]
24. In accordance with claim 19-23 in any one microcapsule encapsulated adsorbent material, characterized in, adsorbent material particles can adsorb small molecule compounds.
[claim25]
25. Method for manufacturing a microcapsule encapsulating an adsorbent material, characterized in,
When the film formed on the microcapsule encapsulating the adsorbent material particles; wherein film having uncharged hydrophilic block and comprising as 1st 1st block of a block copolymer charged polymer, and has a 2nd 1st charged blocks of opposite charge to the charged block has a 2nd polymer;
Comprising:
(A) 1st 2nd polymer will be a party of the adsorbent material particles and the mixing, adsorbed on the adsorbent material pellet;
(B) the step (a) 1st or 2nd polymer mixture with mixing continued for another party, the adsorbent material particles by the 1st and the 2nd polymer formed around a film containing the formed microcapsules, the microcapsules encapsulating a step of making an adsorbent material.
[claim26]
26. In the method according to claim 25, characterized in, this method also includes
(C): cross-linking step (b) 1st/2nd polymer microcapsules which are of a and the step of or.
[claim27]
27. In the method according to claim 25 or 26, characterized in, adsorbent material particles are silica particles.
[claim28]
28. In accordance with the method according to any one of claim 25-27, characterized in, adsorbent material particles have an average particle diameter of 40 nm -10 μm.
[claim29]
29. Method according to any one of claim 25-28, characterized in, this method further comprises the step of adsorbent material particles to surface treatment.
[claim30]
30. Method according to any one of claim 25-29, characterized in, small molecule compounds adsorbed on the adsorbent material particles.
[claim31]
31. A substance encapsulation process for the preparation of microcapsules, characterized in,
When the film formed on the microcapsule encapsulating the target substance, wherein the film contains as having uncharged hydrophilic block and a block copolymer of polymer block charged 1st 1st, and has a band with the 1st 2nd charged blocks charged blocks oppositely charged polymer to 2nd;
Comprising:
(A) as compared to the target substance can be water-soluble high precursor is converted into target substance enzyme, encapsulated in the microcapsules containing the 1st and 2nd polymer formed of a film, a process for encapsulating microcapsules prepare enzyme, and,
(B) compared to a precursor thereof, under conditions of low solubility for the target substance, the precursor to the enzyme encapsulated micro capsule penetration, by enzymes, precursors to the target substance is converted, the target material to precipitate, encapsulated in a microcapsule encapsulated into, a process for preparing microcapsules encapsulating material.
[claim32]
32. In the method according to claim 31, characterized in, within the process (b) are, by mixing an aqueous solution of the enzyme encapsulated microcapsules and precursor, the precursor to the enzyme encapsulated micro capsule penetration.
[claim33]
33. In the method according to claim 32, characterized in, within the process (b) prior to, encapsulated microcapsules with a cross-linking enzyme also including 1st and the 2nd/or polymer process.
[claim34]
34. Microcapsule encapsulating a substance, which is prepared by any one of claim 31-33 method.
[claim35]
35. A low-water-soluble substance encapsulated microcapsules, characterized in,
Than the target substance from a highly water soluble precursor is transformed to obtain a low-water-soluble substance linked to an enzyme of low precursor is transformed into water-soluble substance encapsulated in the microcapsules for formed from film,
Wherein the membrane contains hydrophilic block and having uncharged as 1st 1st block of a block copolymer charged polymer, and has a 2nd 1st charged blocks of opposite charge to the charged block has a 2nd polymer.
[claim36]
36. Water-soluble substance encapsulated microcapsules as those described in accordance with claim 34 or 35, characterized in, with respect to the internal water phase in excess of a low water-soluble substance in a water-soluble substance encapsulated at a concentration of low solubility.
[claim37]
37. In accordance with claim 34-36 sparingly water-soluble substance encapsulated in any one microcapsule, characterized in, 1st and the 2nd/or is cross-linked polymer.
[claim38]
38. Claim 1-4 in any one of a composition comprising a mono-dispersion of microcapsules, and the/or, claim 5, a drug delivery system in any one microcapsules 6, 19-22 and 34-37.
[claim39]
39. A method for delivering a drug to methods that involve, characterized in, which comprises,
(A) microcapsules was formed by the membrane, encapsulation of the drug can be encapsulated microcapsules with a drug precursor into an enzyme preparation step, wherein the membrane contains hydrophilic block and having uncharged as 1st 1st block of a block copolymer charged polymer, and has a 2nd 1st charged blocks of opposite charge to the charged block has a 2nd polymer, and,
(B) a particular site in a subject, the precursor to the enzyme encapsulated micro capsule penetration, by enzymes, converting the precursor is a drug, a step of forming a drug.
[claim40]
40. In the method according to claim 39, characterized in, has low water solubility compared to prodrugs thereof, step (b) are, compared to the precursor exhibits a relatively low solubility of the drug under conditions, precursors to the enzyme encapsulated micro capsule penetration.
[claim41]
41. According to the method described in claim 39 or 40, characterized in, step (b) are, also comprise the drug encapsulated into microcapsules deposited and encapsulated within, the microcapsules encapsulating a step of forming a drug.
  • 出願人(英語)
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • 発明者(英語)
  • KATAOKA KAZUNORI
  • KISHIMURA AKIHIRO
  • ANRAKU YASUTAKA
  • GOTO AKINORI
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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