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NOVEL LIPID FORMULATIONS FOR NUCLEIC ACID DELIVERY
专利权人:
INC.;PROTIVA BIOTHERAPEUTICS
发明人:
MACLACHLAN, IAN,YAWORSKI, EDWARD,LAM, KIEU,JEFFS, LLOYD B,PALMER, LORNE R
申请号:
NZ58858309
公开号:
NZ588583A
申请日:
2009.04.15
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed is a nucleic acid-lipid particle with improved serum stability comprising: A.) A nucleic acid, particularly a small interfering RNA (siRNA); B.) A cationic lipid comprising from 50 mol percent to 65 mol percent of the toal lipid present in the particle; C.) A non-cationic lipid comprising a mixture of a phospholipid and cholesterol or a derivative thereof, wherein the phospholipid comprises from 3 mol percent to 15 mol precent of the total lipid present in the particle and the cholesterol or derivative thereof comprises from 30 mol percent to 40 mol percent of the total lipid present in the particle; and D.) A conjugated lipid that inhibits aggregation of particles comprising from 0.5 mol percent to 2 mol percent of the total lipid present in the particle. Further disclosed is a pharmaceutical composition comprising said nucleic acid-lipid particle and a pharmaceutically acceptable carrier, and the use of said nucleic acid -lipid particle in the manufacture of a medicament for the in vivo delivery of a nucleic acid or for treating a disease or disorder such as viral infection, a liver disease, and cancer.
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