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A kind of ursolic acid polymer drug-loaded nanoparticles and its preparation method and application

A technology of drug-loaded nanoparticles and ursolic acid, which is applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of poor biosafety, poor drug targeting, and wide particle size distribution of drug-loaded nanoparticles. The effect of simple method, controllable delivery, good biocompatibility, and degradability

Active Publication Date: 2021-02-26
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The technical problem to be solved in the present invention is to overcome the defects and deficiencies of the above-mentioned prior art, and provide a kind of ursolic acid polymer drug-loaded nanoparticles, which has a simple preparation method, and the particle size of the drug-loaded nanoparticles is small, uniform and stable, and can realize The positioning and controllable release of drugs in tumor cells has the characteristics of efficient tumor targeting and efficient inhibition of tumor cell growth, and can effectively solve many problems such as wide particle size distribution of drug-loaded nanoparticles, poor drug targeting and poor biological safety.

Method used

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  • A kind of ursolic acid polymer drug-loaded nanoparticles and its preparation method and application
  • A kind of ursolic acid polymer drug-loaded nanoparticles and its preparation method and application
  • A kind of ursolic acid polymer drug-loaded nanoparticles and its preparation method and application

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Embodiment 1

[0065] The synthesis of embodiment 1 PUA

[0066] 1, the following examples use the catalysis of pyridine and thionyl chloride to make polyursolic acid (PUA) through ursolic esterification condensation, comprising the following steps:

[0067] (1) In a well-ventilated environment, add 10 mL of anhydrous pyridine to a clean and dry 25 mL round bottom flask, and stir in an ice bath for 5 min;

[0068] (2) Add 200 μL (2.76 mmol) of thionyl chloride so that the volume ratio of anhydrous pyridine to thionyl chloride is 10:0.2, and stir in an ice bath for 15 minutes;

[0069] (3) Add 0.42g (0.92mmol) UA, so that the molar ratio of thionyl chloride to ursolic acid is 3:1, and the reaction solution is stirred and reacted at room temperature for 1h. After washing and filtering, repeat 3 times to obtain a white filter cake, and freeze-dry to obtain the desired product PUA, 0.35 g (yield: 83.3%).

[0070] The reaction formula of PUA is as follows (n=10):

[0071]

[0072] 2. Result...

Embodiment 2

[0074] The synthesis of embodiment 2 PUA

[0075] Other conditions are identical with embodiment 1, only difference is: control the volume ratio of anhydrous pyridine and thionyl chloride to be 10:0.1, the molar ratio of thionyl chloride to ursolic acid is 1.2:1, and reaction solution is in Stirring and reacting at room temperature for 0.55h, polyursolic acid was successfully prepared.

Embodiment 3

[0076] The synthesis of embodiment 3 PUA

[0077] Other conditions are identical with embodiment 1, only difference is: control the volume ratio of anhydrous pyridine and thionyl chloride to be 10:0.3, the molar ratio of thionyl chloride to ursolic acid is 4.8:1, and reaction solution is in The reaction was stirred for 6 hours at room temperature, and polyursolic acid was successfully prepared.

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Abstract

The invention discloses ursolic acid polymer drug-loading nanoparticles and a preparation method and application thereof. The preparation method includes: subjecting multiple ursolic acid molecules toesterifying reaction through hydroxyl at 3 position and carboxy at 17 position to obtain polyursolic acid; using the polyursolic acid and proper DSPE-PEG2000 to successfully prepare micellar nanoparticles taking the polyursolic acid as a hydrophobic core and hydrophilic chain segment PEG of DSPE-PEG2000 as a shell through a nano precipitation method, in this way, a nano carrier for targeted delivery of antitumor drug is built successfully. The polyursolic acid is taken as a new drug carrier to load hydrophobic antitumor drug, obtained nanoparticles are stable in structure and small in particle size, drug loading capacity can reach 10%, selectivity of the antitumor drug is improved, effectively delivery is realized, and acute toxic and side effect of the antitumor drug is reduced. The preparation method has the advantages of being simple, environment-friendly and economical, and the nanoparticles have great application value in the field of biomedicine.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymer materials and medicaments. More specifically, it relates to a kind of ursolic acid polymer drug-loaded nanoparticle and its preparation method and application. Background technique [0002] At present, the hot spot of nanomedicine is mainly the research on the theoretical delivery pathway and targeting function of pharmaceutical preparations, therapeutic preparations and diagnostic preparations. Especially for tumor targeting, including accurate identification of tumor sites and reduction of side effects. After intravenous administration of anti-tumor nano-drugs, complex interactions (nano-bio interactions) with biological systems (such as proteins, cells, body fluids, tissues and organs, etc.) Antitumor effects of drugs. After the ideal anti-tumor nanomaterial enters the body, it can effectively self-regulate its interaction with the biological system according to the different tiss...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K9/107A61K9/14A61K47/24A61K31/704A61K31/337A61K31/4745A61P35/00
Inventor 吴钧康洋区坤勇
Owner SUN YAT SEN UNIV
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