KR100373844B1 - 유전자 및 생물학적 활성 약물 전달용 양이온성 지질과이의 제조방법 - Google Patents
유전자 및 생물학적 활성 약물 전달용 양이온성 지질과이의 제조방법 Download PDFInfo
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- KR100373844B1 KR100373844B1 KR10-2000-0055399A KR20000055399A KR100373844B1 KR 100373844 B1 KR100373844 B1 KR 100373844B1 KR 20000055399 A KR20000055399 A KR 20000055399A KR 100373844 B1 KR100373844 B1 KR 100373844B1
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- C—CHEMISTRY; METALLURGY
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- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C217/74—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
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- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6905—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
- A61K47/6911—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
- A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
- A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/87—Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
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Abstract
Description
Claims (10)
- 하기 화학식 1로 표시되는 양이온성 지질.화학식 1상기 식에서 y 및 z는 서로 같거나 다른 1 내지 20 사이의 자연수이고; R1∼R5는 서로 같거나 다른 수소, 탄소수 1∼10 사이의 알킬 또는 하이드록시 알킬기, 또는 탄소수 7∼11 사이의 아릴 또는 알알킬기이며; R6은 콜레스테롤 라디칼이고; X는 약학적으로 허용 가능한 할로겐 음이온이다.
- 제1항에 있어서, 상기 X는 Br, Cl 또는 I인 것을 특징으로 하는 양이온성 지질.
- 용매 존재하에서, 콜레스테롤 옥시 유도체에 질소원자를 포함하는 유기염기와 하이드록시 알킬 할라이드를 적가하여 하기 화학식 2로 표시되는 콜레스테롤 옥시 알킬렌 할라이드를 얻은 다음, 이를 용매존재하에서 수소, 또는 한 개 이상의알킬기 또는 하이드록시 알킬기가 치환된 디아민과 반응시킨후, 수소 또는 하이드록시 알킬 또는 알킬 할라이드와 반응시켜 디암모늄염을 생성시키는 것을 특징으로 하는 하기 화학식 1로 표시되는 양이온성 지질의 제조방법.화학식 2X-(CH2)zO-R6화학식 1상기 식에서 y 및 z는 서로 같거나 다른 1 내지 20 사이의 자연수이고; R1∼R5는 서로 같거나 다른 수소, 탄소수 1∼10 사이의 알킬 또는 하이드록시 알킬기, 또는 탄소수 7∼11 사이의 아릴 또는 알알킬기이며; R6은 콜레스테롤 라디칼이고; X는 약학적으로 허용 가능한 할로겐 음이온이다.
- 제3항에 있어서, 상기 콜레스테롤 옥시 유도체는 콜레스테롤 메실레이트인 것을 특징으로 하는 양이온성 지질의 제조방법.
- 제3항에 있어서, 상기 유기염기는 피리딘이고, 상기 하이드록시 알킬 할라이드는 2-브로모에탄올이며, 상기 디아민은 테트라메틸에틸렌디아민인 것을 특징으로 하는 양이온성 지질의 제조방법.
- (a) 다른 지질과 복합체를 형성하는 유효량의 제1항에 따른 양이온성 지질을 포함하는 조성물과 음이온성 분자물질을 접촉시켜 지질 복합체를 형성시키는 단계; 및(b) 상기 지질 복합체와 세포를 접촉시키는 단계를 포함하는 것을 특징으로 하는 세포에 음이온성 분자물질을 전달하는 방법.
- 제6항에 있어서, 상기 조성물이 하나 이상의 부가적인 지질을 포함하는 것을 특징으로 하는 세포에 음이온성 분자물질을 전달하는 방법.
- 제6항에 있어서, 상기 부가적인 지질인 DOPE, DOPC, PC 및 콜레스테롤로 이루어진 군으로부터 하나 또는 그 이상 선택됨을 특징으로 하는 세포에 음이온성 분자물질을 전달하는 방법.
- 제6항에 있어서, 상기 음이온성 분자물질은 DNA, RNA, 단백질, 펩타이드 또는 생물학적 활성 약물인 것을 특징으로 하는 세포에 음이온성 분자물질을 전달하는 방법.
- 제6항에 있어서, 상기 세포가 HeLaS 3, HepG 2, Hep 3B, NIH 3T3, CHRC 2 또는 COS 7인 것을 특징으로 하는 세포에 음이온성 분자물질을 전달하는 방법.
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KR10-2000-0055399A KR100373844B1 (ko) | 2000-09-21 | 2000-09-21 | 유전자 및 생물학적 활성 약물 전달용 양이온성 지질과이의 제조방법 |
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KR20020022868A KR20020022868A (ko) | 2002-03-28 |
KR100373844B1 true KR100373844B1 (ko) | 2003-02-26 |
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Families Citing this family (2)
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KR101198354B1 (ko) * | 2007-10-17 | 2013-03-14 | 주식회사 삼양바이오팜 | 핵산 전달용 저밀도 지단백질 유사(LDL-like) 양이온성 나노입자, 그의 제조방법 및 이를 이용한 핵산의 전달 방법 |
AU2016372321B2 (en) * | 2015-12-18 | 2019-01-24 | Samyang Holdings Corporation | Method for preparing polymeric micelle containing anionic drug |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
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US5283185A (en) * | 1991-08-28 | 1994-02-01 | University Of Tennessee Research Corporation | Method for delivering nucleic acids into cells |
US5650096A (en) * | 1994-12-09 | 1997-07-22 | Genzyme Corporation | Cationic amphiphiles for intracellular delivery of therapeutic molecules |
US5980935A (en) * | 1996-05-15 | 1999-11-09 | Kirpotin; Dmitri | Cationic lipids and methods of use therefor |
US6107286A (en) * | 1994-12-05 | 2000-08-22 | Rhone-Poulenc Rorer S.A. | Lipopolyamines as transfection agents and pharamaceutical uses thereof |
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- 2000-09-21 KR KR10-2000-0055399A patent/KR100373844B1/ko active IP Right Grant
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5283185A (en) * | 1991-08-28 | 1994-02-01 | University Of Tennessee Research Corporation | Method for delivering nucleic acids into cells |
US6107286A (en) * | 1994-12-05 | 2000-08-22 | Rhone-Poulenc Rorer S.A. | Lipopolyamines as transfection agents and pharamaceutical uses thereof |
US5650096A (en) * | 1994-12-09 | 1997-07-22 | Genzyme Corporation | Cationic amphiphiles for intracellular delivery of therapeutic molecules |
US5980935A (en) * | 1996-05-15 | 1999-11-09 | Kirpotin; Dmitri | Cationic lipids and methods of use therefor |
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