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Double-targeting and pH/oxidation reduction double-sensitive core cross-linking nanoparticle as well as preparation method and application

A nanoparticle and dual-targeting technology, which is applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of poor systemic circulation stability, poor targeting, and poor controlled release effect, and achieve controllable release, good stability, and promote quick release effect

Inactive Publication Date: 2018-01-23
TIANJIN POLYTECHNIC UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It aims to improve the targeted delivery efficiency of nanocarriers through the synergistic effect of targeting ligands, cross-linking and pH / redox dual-sensitive hydrophobic cores, and realize the localized and controlled release of drugs in tumor cells to solve the problem of nano-drug carriers. There are many problems such as poor systemic circulation stability, poor targeting and poor controlled release effect

Method used

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  • Double-targeting and pH/oxidation reduction double-sensitive core cross-linking nanoparticle as well as preparation method and application
  • Double-targeting and pH/oxidation reduction double-sensitive core cross-linking nanoparticle as well as preparation method and application
  • Double-targeting and pH/oxidation reduction double-sensitive core cross-linking nanoparticle as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1: FA-P(MApGP) x -b-P(DPA y -co-PDEMA z )(FA-PMgDP) Synthesis of Amphiphilic Block Polymer

[0055] 1) Preparation of 6-O-methacryloyl chloride-1,2:3,4-O-isopropylidene-D-galactopyranose (MAIpGP) monomer

[0056] Under the condition of ice-water bath, add concentrated sulfuric acid (10mL) dropwise into anhydrous acetone (250mL), dissolve evenly, then add D-(+)-galactose (10g) in batches, stir for 0.5h, then stir at room temperature for 5h . Then use saturated NaOH solution to neutralize the pH of the above mixed solution to 7~8, collect the filtrate by filtration and remove the solvent by rotary evaporation, continue to extract with an appropriate amount of ether to collect the ether phase, and pass through anhydrous MgSO 4 Drying and distillation under reduced pressure gave a yellow syrupy liquid; the yellow syrupy liquid was added to a mixed solution of dry tetrahydrofuran (70mL) and dry triethylamine (7mL), and methacryloyl chloride (6mL) was added to the...

Embodiment 2

[0062] Embodiment 2: Preparation of a series of PMgDP block polymers

[0063] The device and steps are the same as in Example 1, except that by adjusting the ratio of DPA, PDEMA monomer and macroinitiator PMAIpGP, a series of block polymers PMgDP with different degrees of polymerization and different hydrophilic-hydrophobic ratios are obtained. As shown in Table 1, the PMgDP polymer is characterized by nuclear magnetic resonance spectroscopy, and the preferred results are as follows figure 1 shown. The characteristic peaks of the polymer PMgDP-III obtained in this example were analyzed, and the results showed that the polymer was successfully synthesized, and the composition was consistent with the feed ratio. The FA-PMgDP-III polymer was characterized by ultraviolet spectroscopy, the results are as follows figure 2 shown. Compared with the UV spectrum of PMgDP-III polymer, FA-PMgDP-III polymer appeared the characteristic peak of folic acid at 362nm, indicating that the po...

Embodiment 3

[0067] Embodiment 3: Preparation of Adriamycin-loaded Nanoparticles

[0068] The polymer FA-PMgDP-III and DOX were co-dissolved in DMSO, and five times the amount of PB solution was dropped into the DMSO mixed solution under the condition of magnetic stirring, and then the solution was loaded into a dialysis bag (MWCO: 3500Da) in the PB solution Dialyzed in medium for 24 hours, and the solvent DMSO was removed to obtain a solution of uncrosslinked drug-loaded nanoparticles.

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Abstract

The invention discloses double-targeting and pH / oxidation reduction double-sensitive core cross-linking nanoparticles as well as a preparation method and application. Hydrophilic layers with folic acid targeting ligand and poly 6O-methyl acryloyl chloride-D-galactopyranose (PMApGP) are arranged on the surfaces of nanoparticles, hydrophobic cores with pH / oxidation reduction double-sensitive polymerunits are arranged inside the nanoparticles, and the hydrophobic cores are cross-linked under the action of dithiothreitol, therefore, stable and reversible double-targeting and pH / oxidation reduction double-sensitive core cross-linking nanoparticles are prepared. Medicine-carrying nanoparticles are prepared from adriamycin as a model medicine, and the stability and the pH / reduction double-sensitivity of medicine-carrying cross-linking nanoparticles can be observed through in-vitro medicine release experiments. Results show that the double-targeting and double-sensitive core cross-linking nanoparticles are simple and convenient in preparation method and high in medicine carrying rate, and the nanoparticles have the properties that the nanoparticles are stable in vitro and low in pH valueinside tumor cells and have hydrophilic-hydrophobic transfer with pH / oxidation reduction sensitive polymer units, and medicines can be rapidly released from a cross-linking structure.

Description

technical field [0001] The invention relates to the fields of polymer chemistry and biomedical engineering, and relates to a double-targeting and pH / redox double-sensitive nuclear cross-linked galactose-based nanoparticle, and a preparation method and application thereof. Background technique [0002] It is well known that cancer treatment is very important to human health as cancer remains one of the leading causes of death worldwide. Among many cancer treatment methods, chemotherapy has become the main strategy for most cancer treatments due to its high efficiency, but most chemotherapeutic agents are released into the blood after administration and non-selectively transported to normal tissues, This usually brings serious toxic and side effects to patients, leading to failure of clinical treatment due to large toxic and side effects, or the inability to increase the dosage due to the limitation of toxic and side effects, so that the ideal therapeutic effect cannot be achi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/22A61K31/704A61P35/00C08F293/00
Inventor 赵军强闫彩霞陈泽李冬阳韩洪蕊冯霞赵义平
Owner TIANJIN POLYTECHNIC UNIV
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