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Lipid nanoparticle membrane material composition

A technology of lipid nanoparticles and lipid nanoparticles, which is applied in the direction of drug combinations, medical preparations of non-active ingredients, organic active ingredients, etc., to achieve the effects of reducing costs, promoting release, and high cell acceptance

Active Publication Date: 2018-04-24
NANJING LUYE PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, if there are a lot of TPGS, it will be difficult for the nanoparticles to be effectively taken up by the target tumor cells because of the steric hindrance effect.

Method used

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  • Lipid nanoparticle membrane material composition
  • Lipid nanoparticle membrane material composition
  • Lipid nanoparticle membrane material composition

Examples

Experimental program
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Effect test

Embodiment 1

[0063] A kind of lipid nanoparticle membrane material composition, described membrane material composition comprises DOTAP, Egg PC, cholesterol, Tween 80, TPGS, and the molar ratio of described membrane material ratio is 25:45:20:5: 5.

[0064] The method for the lipid nanoparticle prepared by above-mentioned lipid nanoparticle membrane material composition, comprises the following steps:

[0065] (1) above-mentioned substance ratio is dissolved in the ethanol of 80%, obtains mixed ethanol solution; Dissolve oligonucleotide G3139 in the PBS damping fluid (1X pH=7), obtain the PBS solution of oligonucleotide; G3139 is a section by Antisense oligonucleotide composed of 18 nucleotides, the nucleotide sequence is 5'-TCT CCC AGC GTG CGC CAT-3';

[0066] (2) Mix the obtained mixed ethanol solution and the PBS solution of oligonucleotide G3139 in equal volumes to obtain a mixed solution with a final ethanol concentration of 40%;

[0067] (3) The 40% final ethanol concentration mixe...

Embodiment 2

[0072] A kind of lipid nanoparticle membrane material composition, described membrane material comprises described membrane material and comprises DOTMA, DOPC, cholesterol, Tween 40, mPEG550-DPPE, and the molar ratio of described membrane material ratio is 35:40 :15:1:1.

[0073] The method for the lipid nanoparticle prepared by above-mentioned lipid nanoparticle membrane material composition, comprises the following steps:

[0074] (1) Dissolve the above-mentioned substance ratio in 80% ethanol to obtain a mixed ethanol solution; dissolve the antisense oligonucleotide G3139 in PBS buffer (1X pH=7) to obtain the PBS solution of the antisense oligonucleotide G3139 ;

[0075] (2) Mix the obtained mixed ethanol solution and the PBS solution of the antisense oligonucleotide G3139 in equal volumes to obtain a mixed solution with a final ethanol concentration of 40%;

[0076] (3) The 40% final ethanol concentration mixed solution obtained in step (2) is further diluted with equal ...

Embodiment 3

[0081] A lipid nanoparticle membrane material composition, the membrane material comprises DDAB, DSPC, cholesterol, Tween 60, mPEG3000-DMPE, and the molar ratio of the membrane material ratio is 30:50:25:3:3 .

[0082] The method for the lipid nanoparticle prepared by above-mentioned lipid nanoparticle membrane material composition, comprises the following steps:

[0083] (1) Dissolving the above substances in 80% ethanol to obtain a mixed ethanol solution; dissolving the antisense nucleic acid in PBS buffer (1X pH=7) to obtain the PBS solution of the antisense nucleic acid G3139;

[0084] (2) Mix the obtained mixed ethanol solution and the PBS solution of the antisense nucleic acid in equal volumes to obtain a mixed solution with a final ethanol concentration of 40%;

[0085] (3) The 40% final ethanol concentration mixed solution obtained in step (2) is further diluted with equal volume of PBS solution; the final ethanol concentration mixed solution is diluted with PBS solut...

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Abstract

The invention discloses a lipid nanoparticle membrane material composition. The membrane material composition consists of cationic lipids, neutral phospholipid, cholesterol, Tween and a polyethylene glycol derivative, wherein the molar ratio of the cationic lipids to the neutral phospholipid to the cholesterol to the Tween to the polyethylene glycol derivative in the membrane material compositionis at (25-35) to (40-50) to (15-25) to (1-5) to (1-5). Meanwhile, the invention also provides a method for preparing lipid nanoparticles by virtue of the lipid nanoparticle membrane material composition. The lipid nanoparticle membrane material composition provided by the invention can improve the stability of the lipid nanoparticles, and subsequently promote the release of drugs in tumor tissuesand reduce the possibility of being degraded.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to a lipid nanoparticle membrane material composition. Background technique [0002] Lipid nanoparticle membrane materials in the prior art do not combine Tween and polyethylene glycol derivatives such as TPGS. For example, Tween is used alone: ​​it has shorter PEG, so that short-chain PEG can increase the gap between nanoparticles. repulsion to prevent its aggregation and reduce stability. On the other hand, due to the lack of long-chain PEG chimera on the surface of nanoparticles, this nanoformulation is easily phagocytized by phagocytic cells, because Tween is easily lost in the systemic circulation. [0003] Another example is the use of polyethylene glycol derivative TPGS alone: ​​although it has a longer PEG chain, it can avoid the recognition of the phagocytic system to a certain extent, and it will not be engulfed by phagocytes and lose its effect, increasing the long circulati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/28A61K47/26A61K47/24A61K47/18A61K31/7088A61P35/00
CPCA61K9/5123A61K9/5146A61K31/7088A61P35/00A61K9/5192A61K31/713
Inventor 程光陈文忠秦利利
Owner NANJING LUYE PHARMA
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