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Preparation method of double-targeting nano microcapsule and anti-tumor application thereof

A nano-microcapsule and dual-targeting technology, which is applied in the direction of anti-tumor drugs, nanocapsules, medical preparations of non-active ingredients, etc., can solve the problems of uneven particle size distribution, uneven product shape, and peptide loading rate Low-level problems, to achieve the effect of uniform shape, high yield and uniform particle size distribution

Inactive Publication Date: 2019-12-20
ANHUI UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The present invention aims to overcome the low drug loading capacity of tripterygium, paclitaxel or docetaxel double-targeted nano-microcapsules, low polypeptide loading rate, uneven product particle size distribution, uneven product appearance and yield in the prior art Low disadvantage, provide a preparation method and anti-tumor application of double-targeted nano-microcapsules

Method used

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  • Preparation method of double-targeting nano microcapsule and anti-tumor application thereof
  • Preparation method of double-targeting nano microcapsule and anti-tumor application thereof
  • Preparation method of double-targeting nano microcapsule and anti-tumor application thereof

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Embodiment 1

[0034] The method for preparing double-targeted nano-microcapsules by applying supercritical fluid-enhanced solution dispersion technology comprises the following steps:

[0035] (1) The volume ratio of dichloromethane, acetone, ethanol and dimethyl sulfoxide is 20:20:5:1, the concentration of tripterine sample is 5mg / mL, the concentration of PLGA is 20mg / mL, Maleimido-PEG2000- The concentration of N-hydroxysuccinimide was 5 mg / mL, and the concentration of RGDCGNKRTRRGD targeting ligand was 0.1 mg / mL. The solution was placed in a magnetic stirring device and stirred at a speed of 100 r / min for 2 hours to obtain a drug mixed solution.

[0036] (2) Adjust the temperature of the high-pressure crystallizer to 35°C, open the carbon dioxide inlet valve of the high-pressure crystallizer, adjust the pressure to 16Mpa, and open the carbon dioxide outlet valve of the high-pressure crystallizer to adjust the CO 2 The volume flow rate reaches 5L / min. After the pressure, temperature, and c...

Embodiment 2

[0039] The method for preparing double-targeted nano-microcapsules by applying supercritical fluid-enhanced solution dispersion technology comprises the following steps:

[0040] (1) The volume ratio of dichloromethane, acetone, ethanol and dimethyl sulfoxide is 20:1:1:1, the concentration of tripterine sample is 5mg / mL, the concentration of PLGA is 20mg / mL, Maleimido-PEG2000-N -The concentration of hydroxysuccinimide is 5 mg / mL, the concentration of RGDCGNKRTRRGD targeting ligand is 0.1 mg / mL, the solution is placed in a magnetic stirring device, and stirred at a speed of 100 r / min for 2 hours to obtain a drug mixed solution.

[0041] (2) Adjust the temperature of the high-pressure crystallizer to 35°C, open the carbon dioxide inlet valve of the high-pressure crystallizer, adjust the pressure to 16Mpa, and open the carbon dioxide outlet valve of the high-pressure crystallizer to adjust the volume flow rate to 5L / min, and wait until the pressure, temperature and carbon dioxide ...

Embodiment 3

[0044] The method for preparing double-targeted nano-microcapsules by applying supercritical fluid-enhanced solution dispersion technology comprises the following steps:

[0045](1) The volume ratio of dichloromethane, acetone, ethanol and dimethyl sulfoxide is 10:5:5:10, the concentration of tripterine sample is 5mg / mL, the concentration of PLGA is 20mg / mL, Maleimido-PEG2000-N -The concentration of hydroxysuccinimide is 5 mg / mL, the concentration of RGDCGNKRTR targeting ligand is 0.1 mg / mL, the solution is placed in a magnetic stirring device, and stirred at a speed of 100 r / min for 2 hours to obtain a drug mixed solution.

[0046] (2) Adjust the temperature of the high-pressure crystallizer to 40°C, open the carbon dioxide inlet valve of the high-pressure crystallizer, adjust the pressure to 8Mpa, and open the carbon dioxide outlet valve of the high-pressure crystallizer to adjust the volume flow rate to 5L / min, and wait for the pressure, temperature and carbon dioxide flow t...

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Abstract

The invention discloses a preparation method of a double-targeting nano microcapsule and anti-tumor application thereof. The method comprises the following steps: (1) dissolving an active ingredient,PLGA, Maleimido-PEG2000-N-hydroxysuccinimide and a targeting peptide in an organic solvent to obtain a mixed solution; (2) adjusting the temperature and the pressure of a crystallization kettle, and opening a CO2 gas outlet valve to adjust the volume flow after the temperature and the pressure of the crystallization kettle are stabilized; (3) spraying the mixed solution into a high-pressure crystallization kettle, maintaining the set temperature and pressure after the injection is finished, and continuously introducing CO2 for 3h or above; and (4) relieving pressure. The method has the advantages of safety, environmental protection, high efficiency and the like. The prepared double-targeting nano microcapsule has high drug loading and high-efficiency capability of targeting and killing glioma cells, has good slow release performance, and can be used as a long-acting injection preparation for targeted treatment of tumor diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method and anti-tumor application of a double-targeting nanometer microcapsule. Background technique [0002] Drug particle size is an important parameter to determine the route of drug administration, especially for the treatment of brain tumors. Due to the existence of the blood-brain barrier (BBB), more than 98% of drugs cannot penetrate the BBB to reach effective lesions. The current broad-spectrum drugs for the treatment of tumors, such as paclitaxel, docetaxel, and tripterine, are difficult to penetrate the BBB to treat brain diseases. However, the supercritical fluid enhanced solution dispersion technology is used to prepare targeted nano-preparations, and the particle size range can be adjusted to 50-800nm ​​by controlling the process parameters, so that the nano-preparations can effectively penetrate the BBB, and at the same time, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/337A61K31/56A61K47/62A61K47/69A61K47/34A61P35/00
CPCA61K9/0019A61K9/5153A61K9/5192A61K31/337A61K31/56A61K47/62A61K47/6925A61P35/00
Inventor 颜庭轩孙玉玺徐霞马亮王肖肖王德强季梦茹赵海莲
Owner ANHUI UNIVERSITY OF TECHNOLOGY