Drug-loading nanoparticles based on ferulic acid polymer, preparation method and applications thereof

A drug-loaded nano-polymer technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, anti-tumor drugs, etc., to achieve the effect of easy operation, simple operation and good repeatability

Active Publication Date: 2019-01-25
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Drug-loading nanoparticles based on ferulic acid polymer, preparation method and applications thereof
  • Drug-loading nanoparticles based on ferulic acid polymer, preparation method and applications thereof
  • Drug-loading nanoparticles based on ferulic acid polymer, preparation method and applications thereof

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Embodiment 1

[0103] The preparation of embodiment 1 polymer PFA

[0104] 1. Prepare the polymer PFA as a drug carrier by the following method, comprising the following steps:

[0105] (1) In an ice-bath environment, add 5 mL of pyridine to adjust the pH to 8-9; stir for 5 min; add quantitative SOCl 2 , stirred for 15 min; added ferulic acid, stirred at room temperature for 1 h; wherein, SOCl 2 The molar ratio with ferulic acid is 1:1;

[0106] (2) Transfer the reddish-brown solution after the reaction to a beaker, add water to precipitate yellow insoluble matter, wash twice with 1% HCl, then wash twice with ultra-pure water, filter to obtain a solid, freeze-dry, and finally obtain brown The powder product is the polymer PFA.

[0107] 2. Results

[0108] (1) The structure of the polymer PFA prepared in Example 1 was characterized by using a 500 M superconducting nuclear magnetic resonance spectrometer (Ascend TM 500) and a Bruker infrared spectrometer (VERTEX70).

[0109] Such as figu...

Embodiment 2

[0113] Example 2 Preparation of a ferulic acid polymer-based nanomaterial PFA nanoparticles

[0114] 1. The preparation of PFA nanoparticles comprises the following steps:

[0115] (1) Prepare PFA with DMSO to make a 10 mg / mL solution, take 200 μL for later use; use DSPE-PEG 3000 as the surface stabilizer, and the dosage of DSPE-PEG 3000 is 50% of the amount of PFA, dissolve in DMSO, take 100 μL spare;

[0116] (2) Mix the above two solutions to obtain 0.3 mL of oil phase, slowly drop it into 3 mL of water phase (water) at 1200 rpm, that is, the volume ratio of water phase to oil phase is 10:1, and stir for 30 s forming a nanoparticle solution;

[0117] (3) Ultrafilter the nanoparticle solution twice (3000 rpm ultrafiltration for 15 min each time) to make the DMSO content below 1 / 1000 to obtain PFA nanoparticles.

[0118] 2. Results

[0119] Characterized by nanopotentiometer and transmission electron microscope, the results show that figure 2 , the prepared nanomaterial...

Embodiment 3

[0120] Example 3 Preparation of drug-loaded nanoparticles based on ferulic acid polymer (PFA@PTX)

[0121] 1. Prepare the drug-loaded nano system by the following method, comprising the following steps:

[0122] (1) Both PFA and paclitaxel (PTX) were prepared into a 10 mg / mL solution with DMSO. Taking the mass ratio of PFA and PTX as 5:1 as an example, 200 μL of PFA and 40 μL of PTX were mixed to obtain the ratio of PFA and PTX Mixed solution; DSPE-PEG 3000 was used as a surface stabilizer, and the amount of DSPE-PEG 3000 was 60% of the amount of PFA. After dissolving in DMSO, 120 μL of DSPE-PEG 3000 solution was mixed with the mixed solution of PFA and PTX above to obtain oil phase;

[0123] (2) Slowly add the mixed oil phase into the water phase (water) at 1200 rpm, control the volume ratio of the water phase to the oil phase to 10:1, and stir for 30 s to form a nanoparticle solution;

[0124] (3) The nanoparticle solution was ultrafiltered twice (3000 rpm ultrafiltration ...

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Abstract

The invention discloses drug-loading nanoparticles based on a ferulic acid polymer, a preparation method and applications thereof. According to the present invention, ferulic acid and SOCl2 are used as raw materials, and are subjected to a condensation polymerization reaction in a pyridine alkaline environment to prepare a polymer PFA, wherein the polymer PFA is non-biotoxic, has good biocompatibility and good degradability, can be prepared into a nanoparticle material, can further be used as a drug carrier for loading hydrophobic drugs, has stable properties, and has a particle size of less than 200 nm; the drug-loading nanoparticles can achieve the long-circulating delivery of anticancer drugs in vivo, are easily permeated and accumulated in the tumor site, and can enhance the targetingeffect of drugs at the tumor site by using the EPR effect so as to enhance the treatment effect and reduce the toxic-side effect on the human body; the preparation method has advantages of simple reaction process, few reaction steps, short reaction cycle, good repeatability and the like; and the drug-loading nanoparticles have good application prospects and broad development space in the medical field.

Description

technical field [0001] The invention belongs to the technical field of drug carriers and controlled release materials. More specifically, it relates to a ferulic acid polymer-based drug-loaded nanoparticle and its preparation method and application. Background technique [0002] Tumor treatment is still a major problem in the current medical field, and it is urgent to develop new anti-tumor drugs and methods with less toxic side effects and significant tumor inhibitory effects. Due to the strong hydrophobicity of most antineoplastic drugs and the existence of a large number of efflux pumps in the gastrointestinal tract, the oral absorption of antineoplastic drugs is poor, and there are generally defects such as low bioavailability and large toxic and side effects. , Improving the bioavailability of anticancer drugs and patient compliance has become an urgent problem to be solved. The biggest obstacle to the administration of antitumor drugs (especially injection administra...

Claims

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Application Information

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IPC IPC(8): C08G63/06A61K9/51A61K47/34A61P35/00
CPCA61K9/5146A61P35/00C08G63/06
Inventor 吴钧郑颖豪游欣如管淑玉顾志鹏
Owner SUN YAT SEN UNIV
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