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Liposome allowing liposome-entrapped substance to escape from endosome

外国特許コード F110005225
整理番号 A252-23WO
掲載日 2011年8月26日
出願国 アメリカ合衆国
出願番号 65286507
公報番号 20070299244
公報番号 8946380
出願日 平成19年1月12日(2007.1.12)
公報発行日 平成19年12月27日(2007.12.27)
公報発行日 平成27年2月3日(2015.2.3)
優先権データ
  • 2005JP012860 (2005.7.12) WO
  • 特願2004-205217 (2004.7.12) JP
発明の名称 (英語) Liposome allowing liposome-entrapped substance to escape from endosome
発明の概要(英語) With the aim of providing a liposome, having a hydrophilic polymer introduced into the outer surface of the liposome membrane, which is a liposome capable of allowing the liposome-entrapped substance to escape from the endosome and be released into the cytoplasm, a liposome membrane component bound to the peptide shown by (a) or (b) below and a liposome membrane component bound to one end of a hydrophilic polymer the other end of which is bound to the peptide shown by (a) or (b) below are included in the liposome: (a) a peptide comprising the amino acid sequence of SEQ ID NO:1; (b) a peptide comprising the amino acid sequence of SEQ ID NO:1 with 1 or more amino acids deleted, replaced or added therein, and capable of fusing lipid membranes with one another under acidic conditions.
特許請求の範囲(英語) [claim1]
1. A liposome comprising: (a) a first liposome membrane component, bound to a first peptide comprising the amino acid sequence of SEQ ID NO:1;
(b) a second liposome membrane component bound to one end of polyethylene glycol the other end of which is bound to a second peptide comprising the amino acid sequence of SEQ ID NO:1, and
(c) a third liposome membrane component bound to one end of polyethylene glycol the other end of which is bound to the substance capable of binding to a receptor or antigen on the surface of a cell membrane,
which liposome is capable of fusing to a cell membrane under acidic conditions,
wherein the second peptide is bound via -- S -- to the other end of polyethylene glycol, and
wherein the liposome is capable of releasing into the cytoplasm an entrapped target substance having a molecular weight ranging from low to high.
[claim2]
2. The liposome according to claim 1, wherein the substance capable of binding to a receptor or antigen on the surface of a cell membrane is transferrin, insulin, folic acid, hyaluronic acid, an antibody or fragment thereof, a sugar chain, a growth factor, or an apolipoprotein.
[claim3]
3. The liposome according to claim 1, further comprising (d) a fourth liposome membrane component bound to one end of polyethylene glycol the other end of which is free.
[claim4]
4. The liposome according to claim 1, encapsulating a target substance to be delivered to the inside of a cell.
[claim5]
5. The liposome according to claim 4, wherein the target substance is a drug, nucleic acid, peptide, protein, sugar, or combinations thereof.
[claim6]
6. The liposome according to claim 1, wherein the liposome is a vector for cellular delivery of a target substance.
[claim7]
7. The liposome according to claim 1, wherein the liposome is a multilamellar vesicle (MLV) or a unilamellar vesicle.
[claim8]
8. The liposome according to claim 7, wherein the unilamellar vesicle is a small unilamellar vesicle (SUV), a large unilamellar vesicle (LUV), or a giant unilamellar vesicle (GUV).
[claim9]
9. The liposome according to claim 1, wherein the liposome is 30 to 100 nm in the diameter.
[claim10]
10. The liposome according to claim 1, wherein the liposome is 50 to 300 nm in diameter.
[claim11]
11. The liposome according to claim 1, wherein the liposome membrane component is selected from the group consisting of a lipid, a membrane stabilizer, an antioxidant, a charged substance, and a membrane protein.
[claim12]
12. The liposome according to claim 11, wherein the lipid is selected from the group consisting of a phospholipid, a glycolipid, a sterol, a saturated fatty acid, and an unsaturated fatty acid.
[claim13]
13. The liposome according to claim 1, wherein the substance capable of binding to a receptor or antigen on the surface of cell membrane is transferrin.
  • 発明者/出願人(英語)
  • CHAKI SHINJI
  • KOGURE KENTARO
  • FUTAKI SHIROH
  • HARASHIMA HIDEYOSHI
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
米国特許分類/主・副
  • 530/303
  • 530/350
  • 530/387.1
  • 530/394
  • 536/22.1
参考情報 (研究プロジェクト等) CREST Creation of Bio-Devices and Bio-Systems with Chemical and Biological Molecules for Medical Use AREA
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