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1. WO2016187935 - DECOY NUCLEIC ACID CATIONIC LIPOSOME CARRIER AND PREPARATION METHOD THEREOF

Publication Number WO/2016/187935
Publication Date 01.12.2016
International Application No. PCT/CN2015/083577
International Filing Date 08.07.2015
IPC
A61K 9/127 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
A61K 31/711 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
711Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 47/42 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/7088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
A61K 31/711
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
711Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 9/0019
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
A61K 9/127
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
A61K 9/1272
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
1271Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
1272with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 江苏凯基生物技术股份有限公司 JIANGSU KEYGEN BIOTECH CORP., LTD [CN]/[CN]
  • 南京艾德凯腾生物医药有限责任公司 NANJING CORE TECH CO., LTD. [CN]/[CN]
Inventors
  • 肖扬 XIAO, Yang
  • 崔进龙 CUI, Jinlong
  • 李正荣 LI, Zhengrong
  • 叶青 YE, Qing
  • 何凌云 HE, Lingyun
  • 王雪根 WANG, Xuegen
Agents
  • 南京苏高专利商标事务所(普通合伙) NANJING SUGAO PATENT AND TRADEMARK FIRM(ORDINARY PARTNERSHIP)
Priority Data
201510268568.622.05.2015CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) DECOY NUCLEIC ACID CATIONIC LIPOSOME CARRIER AND PREPARATION METHOD THEREOF
(FR) SUPPORT DE LIPOSOME CATIONIQUE D’ACIDE NUCLÉIQUE LEURRE ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种Decoy核酸阳离子脂质体载体及其制备方法
Abstract
(EN)
Disclosed is a method for preparing a Decoy nucleic acid cationic liposome carrier. The method comprises the following steps: (1) mixing dioleoyl phosphoethanolamine and (2,3-dioleoyl-propyl)-trimethylamine, and adding an organic solvent into the mixture to obtain a mixed solution; (2) evaporating the mixed solution obtained in step (1) until dry, using an HEPES buffer solution to dissolve the remaining solid fraction, firstly hydrating the solution, and then ultrasonically processing the solution; (3) passing the mixed system obtained after the processing in step (2) through a membrane of 0.4 to 0.8 micrometers, then filtering the mixed system through a membrane of 0.03 to 0.2 micrometers, and preparing a blank liposome; and (4) mixing the blank liposome with protamine and a Decoy nucleic acid, and incubating the mixture to form the Decoy nucleic acid liposome carrier.
(FR)
La présente invention concerne un procédé de préparation d'un support de liposome cationique d’acide nucléique leurre. Le procédé comprend les étapes suivantes : (1) mélange de dioléoyl-phosphoéthanolamine et de (2,3-dioléoyl-propyl)-triméthylamine, et ajout d'un solvant organique dans le mélange pour obtenir une solution mixte ; (2) évaporation de la solution mixte obtenue dans l'étape (1) à sec, en utilisant une solution de tampon HEPES pour dissoudre la fraction solide résiduelle, dans un premier temps par hydratation de la solution, et ensuite par traitement ultrasonore de la solution ; (3) passage du système mixte obtenu après le traitement dans l'étape (2) à travers une membrane de 0,4 à 0,8 micromètre, puis filtration du système mixte à travers une membrane de 0,03 à 0,2 micromètre, et préparation d’un liposome vide ; et (4) mélange du liposome vide avec de la protamine et un acide nucléique leurre, et incubation du mélange pour former le support de liposome d’acide nucléique leurre.
(ZH)
Decoy核酸阳离子脂质体载体的制备方法,包括如下步骤:(1)将二油酰磷脂酰乙醇胺和(2,3-二油酰基-丙基)-三甲胺混合,加入有机溶剂溶解得到混合溶液;(2)将步骤(1)得到的混合溶液蒸干,使用HEPES缓冲液溶解剩余的固体部分,先水合,再超声;(3)将步骤(2)处理后得到的混合体系先过0.4~0.8μm的膜,再过0.03~0.2μm的膜,制备空白脂质体;(4)将空白脂质体与鱼精蛋白、Decoy核酸混合,孵育形成Decoy核酸阳离子脂质体载体。
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Latest bibliographic data on file with the International Bureau