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PH-sensitive polymandelic acid nano-drug carrier, and preparation method and application thereof

A nano drug, mandelic acid technology, applied in the field of biomedicine, can solve the problem of low bioavailability, achieve good biocompatibility, good pH responsiveness, and improve the effect of bioavailability

Active Publication Date: 2018-12-18
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The nano-drug carrier can realize the loading of hydrophobic drugs, which not only overcomes the disadvantages of poor solubility and low bioavailability of hydrophobic drugs in water, but also has strong sensitivity to environmental pH, and the carrier itself has the pharmacological properties of inhibiting tumors. Activity and good biocompatibility can help improve the therapeutic effect of tumor drugs, and open up a new way for the effective treatment of tumors

Method used

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  • PH-sensitive polymandelic acid nano-drug carrier, and preparation method and application thereof
  • PH-sensitive polymandelic acid nano-drug carrier, and preparation method and application thereof
  • PH-sensitive polymandelic acid nano-drug carrier, and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0052] The preparation of embodiment 1 polymer PMA

[0053] 1, the preparation of polymer PMA, comprises the following steps:

[0054] (1) Mix 5 mL of pyridine, 400 µL of thionyl chloride SOCl 2 and 1.676 g of mandelic acid were put into a round-bottomed flask, and reacted at room temperature (24-25°C) for 2 h under stirring conditions;

[0055] (2) After the drug crystals gradually disappear and a red transparent viscous liquid appears, add 150 mL of ultra-pure water, and let it stand for precipitation to obtain a solid, which is a preliminary polymerization product;

[0056] (3) Add ultrapure water to the preliminary polymerization product obtained by precipitation, and wash it several times until there is no peculiar smell, then add 150 mL ultrapure water for ultrasonic washing (washing at least 3 times, each time for more than 0.5 h), Then vacuum suction filtration, and the suction filtration product is freeze-dried to obtain the polymer PMA (polymandelate).

[0057] 2....

Embodiment 2

[0061] Example 2 Preparation of a pH-sensitive drug-loaded nanoparticle PTX@NPs

[0062] 1. Preparation of drug-loaded nanoparticles PTX@NPs, including the following steps:

[0063] (1) Stir 3 mL of ultrapure water in a glass bottle (1500 rpm);

[0064] (2) Add 300 µL of 15 mg / mL polymer PMA, 150 µL of 15 mg / mL DSPE-PEG and 50 µL of 15 mg / mL paclitaxel (PTX) in the solvent dimethyl sulfoxide After dissolving and mixing, a mixed oil phase material is obtained;

[0065] (3) Add 500 µL of mixed oil phase material (the volume ratio of water phase and oil phase is 6:1) dropwise to the glass bottle in step (1), take it out after 60 seconds and transfer it Centrifuge at constant volume in an ultrafiltration centrifuge tube (2500 rpm, 8 min), and wash with ultrafiltration for 3 times to obtain drug-loaded nanoparticles PTX@NPs.

[0066] 2. Characteristic analysis of drug-loaded nanoparticles PTX@NPs

[0067] Analyzed by DLS, by figure 2 It can be seen that the particle size of t...

Embodiment 3

[0075] The preparation of embodiment 3 polymer PMA

[0076] Other conditions are the same as in Example 1, the only difference is: pyridine (analytical grade, 1 mL), thionyl chloride SOCl 2 (100 µL) and mandelic acid (1 g) were put into a round bottom flask and stirred at room temperature for 2 h.

[0077] According to infrared analysis, this example adopts the solution polymerization method to obtain the polymer PMA by one-step polycondensation, and finally obtains drug-loaded nanoparticles with a uniformly dispersed spherical structure, which can be rapidly decomposed in the acidic microenvironment of tumor cells, so that paclitaxel can be deposited on the tumor site. It can be released more quickly, so as to achieve a more effective anti-tumor effect.

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Abstract

The invention discloses a pH-sensitive polymandelic acid nano-drug carrier, and a preparation method and an application thereof. A polyester material synthesized in the invention has good biocompatibility, and can be used as the nano-drug carrier to carry a hydrophobic drug to improve the bioavailability of the hydrophobic drug; the carrier has a tumor inhibition pharmacological activity, and canbe combined with an anticancer drug to achieve a better anticancer effect; and the nano-drug carrier has good pH response in a tumor cell acidic micro-environment to make the antitumor drug quickly released in tumor sites, can help to improve the treatment of the anticancer drug on the tumors, has a protection effect on the anticancer drug, and can prevent the antitumor drug from being prematurelyreleased in other sites. The nano-drug carrier has the advantages of simple reaction process, few reaction steps, short reaction period and high repeatability, and has a good application prospect anda broad development space in the medical field.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to a pH-sensitive polymandelic acid nano drug carrier and its preparation method and application. Background technique [0002] Polyester polymers are an important class of biomedical nanomaterials, which have good biocompatibility and excellent biodegradability, and have the advantages of being non-toxic, harmless, cheap and widely used, and have good application prospects in the field of drug delivery and Broad room for development. There are many traditional methods for synthesizing polyester polymers, among which the direct polycondensation method is one of the main methods for synthesizing polyester materials. The direct polycondensation method includes melt polymerization and solution polymerization. Melt polycondensation reacts at a temperature higher than the melting point of the polymer, but conditions such as reaction temperature, time, and vacuum are...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/06C08G63/78A61K47/34A61K31/337A61P35/00
CPCA61K31/337A61K47/34A61P35/00C08G63/065C08G63/78
Inventor 吴钧宋春丽温惠云游欣如顾志鹏
Owner SUN YAT SEN UNIV
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