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Ph-responsive morphology reversible change polymer micelles and preparation method and application

A polymer glue and polymer technology, which can be used in medical preparations without active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of low solubility and low bioavailability, and improve the release concentration. , Increase the solubility, the effect of not easy to release

Active Publication Date: 2022-05-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dabigatran etexilate capsules currently used in the market are oral preparations, which are only used as antithrombotic agents and belong to BCSⅡclass II drugs, with low solubility and low bioavailability

Method used

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  • Ph-responsive morphology reversible change polymer micelles and preparation method and application
  • Ph-responsive morphology reversible change polymer micelles and preparation method and application
  • Ph-responsive morphology reversible change polymer micelles and preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Synthesis of mPEG-PLA: Add mPEG2000 (25g) and D, L-lactide (27g) into a 100ml dry two-necked bottle, vacuumize, fill with nitrogen, repeat 3 times to ensure that the reaction system is anhydrous and oxygen-free, and Place the two-necked bottle in an oil bath, slowly heat up to 135°C, and when the material is completely dissolved and the temperature drops to 110°C, add a catalyst of 0.2% (W / V) of stannous octoate. In order to quickly add the catalyst, stannous octoate Dilute with toluene according to a certain ratio, quickly add a certain amount of catalyst under the condition of nitrogen flow, then seal the system, vacuumize, fill with nitrogen, repeat three times, raise the temperature of the reaction system to 145 ° C, and react for 6 hours. After the reaction, cool the two-necked bottle to room temperature, open the sealing device, add an appropriate amount of dichloromethane to dissolve, precipitate the product with glacial ether, filter, and repeat 3 times to obtain...

Embodiment 2

[0045] The prepared mPEG-PLA, mPEG-PLA-(HE) in Example 1 6 CC and mPEG-PLA-(RG) 6 The CC carrier is fed according to the mass ratio of 10:0.8:1.2, and the drug is dabigatran etexilate, wherein the ratio of the total mass of the carrier to the drug is 20:1, adding an organic reagent to dissolve the carrier and the drug, spinning the organic reagent to dry, and hydrating , passed through a 0.22 or 0.45 μm water film, exposed to the air, and freeze-dried to obtain a pH-responsive polymer micelle with a reversible change in shape.

Embodiment 3

[0049] The effect of different pH values ​​on the particle size of polymer micelles was investigated. mPEG-PLA-(HE) 6 CC and mPEG-PLA-(RG) 6 Weigh an appropriate amount of CC carrier according to the molar ratio of 1:1, dissolve it with Hepes buffer solution with pH 7.4, measure the particle size, then adjust the pH to 6.5 with acetic acid, then adjust the pH to 7.4 with ammonia water, and finally adjust the pH to 7.4 with acetic acid. pH to 6.0, measure the particle size of the polymer micelle micelles under different pH conditions with a particle size meter, such as Figure 8 As shown, the particle size of polymer micelles changes with the change of pH.

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Abstract

The invention discloses a polymer micelle with a pH-responsive shape reversible change, a preparation method and an application thereof. The polymer micelle is respectively connected with different amino acid sequences by the hydrophobic ends of the amphiphilic polymer, and the amino acid sequence ends Containing disulfide bonds, the amino acid sequence is pH-responsive. In the present invention, electrostatic adsorption occurs in a normal physiological environment, the micelle core is relatively tight, and at the same time, the disulfide bonds are cross-linked, and the micelle is more stable. In the tumor microenvironment, the amino acid sequence of the micelle core is protonated and positively charged. Electrostatic repulsion occurs with another polypeptide, and the core of the polymer micelle expands, but due to the effect of disulfide bond cross-linking, the micelle will not disintegrate. If the micelle leaves the tumor microenvironment, the micelle shrinks, reducing the release of the drug, thereby Reduce the damage of drugs to normal cells; in addition, apply dabigatran etexilate to the direction of tumors, and provide direction for the combination therapy of dabigatran etexilate and chemotherapy drugs in the future.

Description

technical field [0001] The invention relates to tumor-targeting drugs, in particular to a pH-responsive polymer micelle with reversible change in shape, its preparation method and application. Background technique [0002] In recent years, nanoparticles have shown great potential, among which liposomes, polymer micelles, and albumin nanoparticles have marketed drugs, but due to the complexity of the tumor microenvironment, there are still huge obstacles in the delivery of nanoparticles, such as Abnormal vasculature reduces the opportunity for nanoparticles to enter the tumor area, the dense extracellular matrix hinders the entry of nanoparticles into the tumor tissue, and the high interstitial pressure easily pumps the nanoparticles entering the tumor tissue out of the blood. Barriers to the delivery of nanoparticles. Studies have shown that the particle size of nanoparticles will affect the penetration and retention of nanoparticles in tumor sites. In order to increase the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4439A61K47/34A61P35/00C08G63/91C08G63/664
CPCA61K9/1075A61K31/4439A61K47/34A61P35/00C08G63/912C08G63/664
Inventor 孙春萌涂家生孙梦娟
Owner CHINA PHARM UNIV
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