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Macrolides compound and siRNA-containing composition and preparation method thereof

A compound and macrocyclic ester technology, applied in the field of medicine and biology, can solve the problems of strong inflammatory response, difficult to pass through the cell membrane, short half-life, etc., to reduce adverse reactions, improve pharmacokinetic characteristics, and change biodistribution. Effect

Active Publication Date: 2015-09-30
厦门成朴希晟股权投资合伙企业(有限合伙)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Naked siRNA itself is negatively charged, has a large molecular weight, and strong polarity. It is difficult to pass through the cell membrane and vascular endothelium, and it is easy to stay in the spleen. It is easily degraded by nucleases in vivo, with a short half-life, low transfection efficiency, and even strong inflammation. reaction etc.

Method used

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  • Macrolides compound and siRNA-containing composition and preparation method thereof
  • Macrolides compound and siRNA-containing composition and preparation method thereof
  • Macrolides compound and siRNA-containing composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 synthetic compound T2C1 compound

[0030] Weigh 100 mg of 1,4,7,10-tetraazacyclododecane and mix it with 726.8 mg of C12-14-alkyl glycidyl ether, and then incubate at 92°C for 43 hours to synthesize T2C1.

Embodiment 2

[0032] Preparation formula siRNA (siRNA+T2C1+cholesterol-polyethylene glycol+DPPE 1:1:1:1)

[0033] Preparation of preparation: Weigh a certain amount of 100mg T2C1, cationic lipid DOTMA, phospholipid DPPE, cholesterol-polyethylene glycol cholesterol polyethylene glycol, mix and dissolve in chloroform in a glass container, remove chloroform under vacuum . Then add 300ml of water, vortex and oscillate to dissolve in water, after homogenization treatment, the homogenization condition is 1000 bar, two cycles (ATS homogenizer).

Embodiment 3

[0035] siRNA: T2C1 cholesterol-polyethylene glycol: DPPE is 1:0.3:0.3:0.4.

[0036] Preparation of preparation: Weigh a certain amount of 100mg T2C1, cationic lipid DOTMA, phospholipid DPPE, cholesterol-polyethylene glycol, mix and dissolve in ethanol in a glass container, and remove ethanol under vacuum. Then add 300ml of water, vortex and oscillate to dissolve in water, after homogenization treatment, the homogenization condition is 1000 bar, two cycles (ATS homogenizer).

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Abstract

The invention belongs to the biological medicine field, and more specifically relates to a macrolides compound and siRNA-containing composition and a preparation method thereof. The composition comprises a siRNA sequence and the macrolides compound, and also comprises one or combination of more than two of cation lipid, phosphatide and cholesterol-polyethylene glycol. The macrolides compound and siRNA-containing composition can increase the pharmacokinetics characteristic for siRNA treatment, is capable of changing bio-distribution, intracellular intake, targeting property and transfection efficiency, and reducing adverse reaction.

Description

technical field [0001] The invention belongs to the field of medicine and biology, and specifically relates to a composition comprising a macrocyclic ester compound and siRNA and a preparation method thereof. Background technique [0002] Since the discovery of RNA interference (RNAi) technology more than 10 years ago, RNAi has become a key regulator of cytogenetics and a powerful tool for elucidating the growth, pathogenesis and aging of organisms. The siRNA binds to the associated protein to form RNA. RISC recognizes and degrades the messenger RNA (messenger RNA, mRNA) of the target gene through the guidance of siRNA, so that the expression of specific protein is inhibited, and then specifically leads to gene silencing. The key to the success of RNAi lies in whether siRNA can be completely transfected into target cells and combined with target gene mRNA, and the stability of siRNA in vivo is of great significance. Studies have shown that chemical modification of siRNA st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K48/00A61K47/22A61P1/16A61P31/20
Inventor 崔坤元梁东陈波
Owner 厦门成朴希晟股权投资合伙企业(有限合伙)
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