Nano drug-loading system based on poly-salicylic acid, and preparation method and application thereof

A technology of polysalicylic acid and nano-drug-loading, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. and other problems, to achieve the effect of enhanced drug aggregation, good biological safety, and simple preparation method.

Active Publication Date: 2018-12-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But there are two disadvantages in salicylic acid: the one is that two molecules of salicylic acid can form intermolecular hydrogen bonds, which will affect the biosynthesis effect of cells, and the solubility of salicylic acid in water is not high; biological toxicity

Method used

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  • Nano drug-loading system based on poly-salicylic acid, and preparation method and application thereof
  • Nano drug-loading system based on poly-salicylic acid, and preparation method and application thereof
  • Nano drug-loading system based on poly-salicylic acid, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The preparation of embodiment 1 polysalicylic acid

[0067] 1. The preparation of polysalicylic acid (PSA), comprising the following steps:

[0068] (1) In an ice-bath environment, add 15 mL of anhydrous pyridine to a 50 mL round bottom flask and stir for 5 min; slowly add 10 mmol of thionyl chloride dropwise to anhydrous In pyridine, stir for 15 min;

[0069] (2) Add 20 mmol salicylic acid at one time, stir and react at room temperature for 1 h;

[0070] (3) After the reaction was completed, deionized water was dropped to terminate the reaction; the obtained mixture was suction-filtered, washed several times with deionized water, and freeze-dried to obtain a white powdery solid, which was polysalicylic acid (PSA).

[0071] 2. Results

[0072] figure 1 It is the infrared spectrogram of the prepared polysalicylic acid. From figure 1 It can be seen that the carbonyl absorption peak in COOH (purple) on SA after polymerization is red-shifted to the absorption peak of ...

Embodiment 2

[0073] Example 2 Preparation of a polysalicylic acid-based nano-drug loading system (DTX@PSA NPs)

[0074] The preparation of a nano drug loading system (DTX@PSA NPs), comprising the following steps:

[0075] (1) Dissolve polysalicylic acid, docetaxel and DSPE-PEG 2000 in DMSO respectively, prepare a solution with a concentration of 20 mg / mL, and pass through a 0.22 μm filter membrane;

[0076] (2) After mixing 200 µL of polysalicylic acid solution, 50 µL of DTX solution and 40 µL of DSPE-PEG 2000 solution, the organic phase was obtained; at a stirring speed of 800 rpm, 290 µL of the organic phase was added dropwise to 3 mL of water, stop stirring after the dropwise addition is completed;

[0077] (3) Centrifuge the resulting mixed solution to remove DMSO with an ultrafiltration tube at a speed of 2500 rpm for 8 to 10 minutes, wash with deionized water, and repeat twice to obtain a suspension that is polysalicyl Drug-loaded acid nanoparticles (DTX@PSANPs).

Embodiment 3

[0078] Example 3 Quality evaluation of drug-loaded nanoparticles (DTX@PSA NPs)

[0079] (1) Appearance of the nano drug-loaded particles prepared in Example 2: relatively clear with light blue opalescence.

[0080] (2) Morphological observation of the nano-drug loading system: combining figure 2 As shown, the nano-drug-loaded particles of Example 2 prepared by the nano-precipitation method were regular in shape and uniform in size as observed by transmission electron microscopy.

[0081] (3) Stability evaluation of the nano drug-loaded system: the nano drug-loaded particles prepared in Example 2 were respectively dispersed in PBS and PBS containing 10% FBS, as shown in image 3 As shown, the particle size did not change much within 7 days, and basically remained at about 60 nm.

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Abstract

The invention discloses a nano drug-loading system based on poly-salicylic acid, and a preparation method and application thereof. Salicylic acid serving as a monomer is rapidly and conveniently prepared into poly-salicylic acid macromolecules according to a one-step polycondensation method; the poly-salicylic acid macromolecules cover hydrophobic antitumor drugs through self-assembly to form thenano drug-loading system. The drug-loading system has high biocompatibility, moderate size and uniform particle diameter, drug aggregation in tumors can be maintained by the enhanced permeability andretention effect (EPR) of tumor tissues, the bioavailability and the curative effect of the drugs are improved, and a new approach for effective treatment of cancers and other diseases is provided; the nano drug-loading system has the advantages of simple reaction process, few reaction steps, short reaction period, high repeatability and the like, thereby having a good application prospect and a broad development space in the medical field.

Description

technical field [0001] The invention belongs to the technical field of nanometer materials. More specifically, it relates to a polysalicylic acid-based nano drug-carrying system and its preparation method and application. Background technique [0002] At present, malignant tumors, together with cardiovascular diseases and respiratory diseases, have become the three diseases with the highest mortality rate. Traditional tumor treatment methods mainly include surgery, chemotherapy, radiotherapy and traditional Chinese medicine treatment, among which chemotherapy is the most important method. However, due to the strong hydrophobicity of most anticancer drugs and the existence of a large number of efflux pumps in the gastrointestinal tract, the oral absorption of anticancer drugs is poor, and chemotherapy drugs generally have low bioavailability and severe side effects. Therefore, improving the bioavailability of chemotherapy drugs and patient compliance has become an urgent pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/06A61K47/34A61K45/00A61P35/00
CPCA61K45/00A61K47/34A61P35/00C08G63/065
Inventor 吴钧游欣如顾志鹏
Owner SUN YAT SEN UNIV
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