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ph and oxidation-reduction dual-sensitive layer cross-linking nanoparticle as well as preparation method and application thereof

A nanoparticle, sensitive technology, applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of fast clearance rate, poor targeting, poor controlled release effect, etc., to achieve improved enrichment and retention, low toxicity, and biocompatibility good sex effect

Active Publication Date: 2014-12-24
天津渤化讯创科技有限公司
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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 groups, hydrophilic segments, disulfide bond reversible cross-linked shells, and pH-sensitive hydrophobic cores, and realize the controlled release of drugs in tumor cells. In order to solve many problems such as fast systemic circulation clearance rate, poor targeting, and poor controlled release effect of nano drug carriers in the prior art

Method used

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  • ph and oxidation-reduction dual-sensitive layer cross-linking nanoparticle as well as preparation method and application thereof
  • ph and oxidation-reduction dual-sensitive layer cross-linking nanoparticle as well as preparation method and application thereof
  • ph and oxidation-reduction dual-sensitive layer cross-linking nanoparticle as well as preparation method and application thereof

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Experimental program
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Embodiment 1

[0047] figure 1 It is a schematic diagram of double sensitive layer cross-linked nanoparticles of the embodiment of the present invention. from figure 1 It can be seen from the figure that the double sensitive layer cross-linked nanoparticles of the present invention have a three-layer structure, the outer layer is RGD with tumor targeting function and zwitterionic polymer PCB, the middle layer is a disulfide bond cross-linked shell layer, hydrophobic The drug is loaded in the inner core through the hydrophobic interaction with the hydrophobic segment PDPA. Example 1 (I-1)

[0048] The preparation method of triblock RGD-PCB-b-PDS-b-PDPA polymer comprises the steps:

[0049] (a) Preparation of PCB(tBU)-b-PDS-b-PDPA polymer

[0050] Add the reversible addition-fragmentation chain transfer polymerization (RAFT) chain transfer agent trithiododecyl-2-isopropionate (CTAm) (36.5 mg, 0.1 mM) and zwitterionic monomer in the shlenk reaction tube in sequence Carboxybetaine tert-buty...

Embodiment 2～ Embodiment 12

[0060] Device and operation are with embodiment 1, just by adjusting carboxylate betaine tert-butyl methyl methacrylate (CB-tBU), methacrylamide ethyl pyridine disulfide (DS) and methacrylic acid diisopropylamino The ratio of monomers such as ethyl ester (DPA) and chain transfer agent trithiododecyl-2-isopropionate (CTAm) obtains three-block polymers with different degrees of polymerization, as shown in Table 1:

[0061] Table 1: pH- and redox-sensitive polymers

[0062]

[0063] N a is the molar ratio of RGD to PCB-b-PDS-b-PDPA triblock polymer.

Embodiment 13

[0064] Embodiment 13 (I-13):

[0065] According to the method and device of Example 1 (a), replace CB-tBU with polyethylene glycol acrylate (RGD-PEG480-AC) bonded by RGD, and the number average molecular weight of the polyethylene glycol segment is 480 to obtain RGD-PEG480-AC. b-PDS-b-PDPA. NMR characterization of its composition RGD-PEG480 10 -b-PDS 10 -b-PDPA 25 (I-13), the subscript is the degree of polymerization of the corresponding monomer.

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Abstract

The invention relates to a pH and oxidation-reduction dual-sensitive layer cross-linking nanoparticle as well as a preparation method and an application thereof. A hydrophilic layer which at least contains PCB (Polycarboxylate Betaine) or PEG (Polyethylene Glycol) is positioned on the surface of the nanoparticle, a hydrophobic nuclei which at least contains a pH-sensitive polymer unit is positioned in the nanoparticle, and an S-S (Disulfide Bond) cross-linking layer which is formed through cross-linking reaction between PDS (Polymethacrylamide Ehtylpyridine Disulfide) units is positioned between the hydrophilic layer and the hydrophobic nuclei. A tumor targeted group can be modified on the hydrophilic layer positioned on the surface of the pH and oxidation-reduction dual-sensitive layer cross-linking nanoparticle, and the gathering of the nanoparticle on a tumor tissue and the endocytosis of the nanoparticle on the tumor cell are accelerated through the specific targeted effect of the nanoparticle on a tumor cell. The pH and oxidation-reduction dual-sensitive layer cross-linking nanoparticle disclosed by the invention has the advantages of good biocompatibility and low toxicity. According to the pH and oxidation-reduction dual-sensitive layer cross-linking nanoparticle, a cross-linked structure is dissociated under the action of glutathione inside the tumor cell, so that the release of a medicine is promoted. The preparation method disclosed by the invention is simple, convenient, good in stability and conveniently operated and popularized.

Description

technical field [0001] The invention relates to the fields of polymer chemistry and biomedical engineering, in particular to a cross-linked nanoparticle of a pH- and redox-sensitive polymer layer, a preparation method and application thereof. Background technique [0002] At present, cancer (ie, malignant tumor) is one of the diseases with high morbidity and mortality in the world. Chemotherapy is one of the most important treatment methods in many cancer treatments, but the delivery of anti-tumor drugs to tumor cells is seriously hindered due to the clearing effect of the systemic circulation, low permeability of tumor tissues, and drug resistance of tumor cells. efficiency, leading to poor efficacy. In addition, the existing anti-tumor drugs have serious side effects on normal tissues while killing tumor cells, leading to the failure of clinical treatment due to the large side effects, or the inability to increase the dose due to the limitation of side effects, so that th...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F8/30A61K9/51A61K47/42A61K47/34A61P35/00A61K47/10
Inventor 董岸杰黄平升邓联东
Owner 天津渤化讯创科技有限公司
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