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Targeted lipidosome drug-loading system containing aptamers, preparation method and application

A technology of targeting liposome and drug-carrying system, which is applied in the field of aptamer-targeting liposome drug-carrying system and preparation, can solve problems such as low stability, achieve protection and stability, increase drug enrichment, and improve The effect of antitumor effect

Inactive Publication Date: 2016-04-20
GUANGXI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide an aptamer-targeted liposome prepared using sphingomyelin for the defect of low stability of the drug-carrying system of the aptamer-targeted liposome prepared by conventional phospholipids Drug-loading system, preparation method and application

Method used

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  • Targeted lipidosome drug-loading system containing aptamers, preparation method and application
  • Targeted lipidosome drug-loading system containing aptamers, preparation method and application
  • Targeted lipidosome drug-loading system containing aptamers, preparation method and application

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preparation example Construction

[0039] The present invention also provides preparation steps and parameters of suitable aptamer-targeted liposome drug delivery system for sphingomyelin, because the chemical structure and hydrophilicity of different phospholipids are different, other methods in the prior art The steps and parameters for preparing the aptamer targeting liposome drug delivery system from phospholipids are not fully applicable to the present invention. see figure 1 , as the preparation method of the aptamer-targeted liposome drug-carrying system according to the preferred embodiment of the present invention, the aptamer-targeted liposome drug-carrying system as described above can be prepared. As shown in the figure, the preparation method includes:

[0040] First, in step S1, the sphingomyelin component, the cholesterol component, the phospholipid stabilizer and the functional phospholipid are dissolved in an organic solvent at a molar ratio of 50-60:35-45:4-5:0.2-0.4 to prepare a blank lipid ...

Embodiment 1

[0054] In Example 1, the aptamer targeting liposome drug delivery system sgc8 / VCR-Lipo was prepared.

[0055] Preparation of S1, PEG long-circulating liposome (Lipo):

[0056] Egg sphingomyelin (SM), cholesterol (Cholesterol), DSPE-PEG2000 and DSPE-PEG2000-MAL dissolved in chloroform were added into a round-bottomed flask at a molar ratio of 55:40:4.7:0.3, and heated at 60°C with The rotary evaporator rotates at a speed of 200 rpm / min and turns on the vacuum pump to vacuum for 10 minutes to form a dry film, and the vacuum dryer is dried overnight to remove residual organic solvents.

[0057] Among them, SM is the product of Avantipolarlipids, the product number is 860061P; cholesterol is the product of Avantipolarlipids, the product number is 700100P; DSPE-PEG2000 is the product of Avantipolarlipids, the product number is 880128P; DSPE-PEG2000-MAL is the product of Avantipolarlipids, the product number is 880126P.

[0058]The lipid film at the bottom of the bottle was hydrate...

Embodiment 2

[0064] In Example 2, the aptamer targeting liposome drug delivery system sgc8 / VCR-Lipo was prepared.

[0065] Preparation of S1, PEG long-circulating liposome (Lipo):

[0066] Egg sphingomyelin (SM), cholesterol (Cholesterol), DSPE-PEG2000 and DSPE-PEG2000-MAL dissolved in chloroform were added into a round-bottomed flask at a molar ratio of 50:45:5:0.2, and heated at 70°C with The rotary evaporator rotates at a speed of 100 rpm / min and turns on the vacuum pump to vacuum for 20 minutes to form a dry film, and the vacuum dryer is dried overnight to remove residual organic solvents.

[0067] Wherein the raw material SM, cholesterol, DSPE-PEG2000 and DSPE-PEG2000-MAL selected products are the same as in Example 1.

[0068] The lipid film at the bottom of the bottle was hydrated with 1 ml of 300 mM citrate buffer (pH=4.0), ultrasonicated in a 60°C water bath for 30 min, and then repeatedly frozen and thawed in liquid nitrogen and a 50°C water bath for 6 times. The product is pac...

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Abstract

The invention relates to a targeted lipidosome drug-loading system containing aptamers and a preparation method of the system. The targeted lipidosome drug-loading system containing the aptamers comprises the aptamers, an antitumor drug and nano-liposomes prepared from sphingomyelin, wherein the antitumor drug is wrapped with the nano-liposomes and the aptamers are connected onto the nano-liposomes through chemical bonds for specifically identifying tumor cells. The nano-liposomes are prepared from sphingomyelin and are connected with an appropriate quantity of the aptamers after the antitumor drug is wrapped with the nano-liposomes, sphingomyelin contains more amido bonds and can resist chemical and biological degradation better, protect stability of a lipidosome structure and increase the drug accumulation content of the tumor cells, and accordingly, the antitumor effect is improved.

Description

technical field [0001] The invention relates to a targeted drug delivery system for cancer, more specifically, to an aptamer-targeted liposome drug delivery system, a preparation method and application. Background technique [0002] Liposome, a closed vesicle with bilayer structure formed by phospholipids or other lipid compounds, is a non-viral carrier with stable properties and long half-life in blood circulation. Encapsulating anti-tumor drugs in liposomes can not only protect the drugs from decomposition by body enzymes before entering the lesion site, prolong the drug circulation time, increase the concentration and action time of the drug at the lesion site, improve curative effect, and reduce toxicity; Moreover, compared with other delivery systems, liposomes can provide superior biocompatibility, biodegradability, low toxicity, size controllability and surface functional modification. [0003] Although the liposome preparation of antineoplastic drugs delivers high e...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/48A61K47/24A61K47/34A61K31/475A61K31/704A61K33/24A61K31/337A61P35/00
CPCA61K47/24A61K31/337A61K31/475A61K31/704A61K33/24A61K47/10
Inventor 卢小玲赵永祥
Owner GUANGXI MEDICAL UNIVERSITY
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