Preparation method and application of nano-drug carrier with long circularity

A nano-drug carrier, long-circulation technology, applied in nano-drugs, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Side effects and other problems, to achieve the effect of improving bioavailability, immunogenicity, antibacterial and anticancer, and reducing the number of drugs

Pending Publication Date: 2021-05-14
XI'AN POLYTECHNIC UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Chemotherapy drugs widely used in clinical practice are widely distributed in the body, especially in some normal tissues, which not only reduces the bioavailability of drugs, but also causes significant side effects on normal tissues
In addition, the circulation time of the drug in the blood is too short, and it is difficult to reach the lesion site

Method used

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  • Preparation method and application of nano-drug carrier with long circularity
  • Preparation method and application of nano-drug carrier with long circularity
  • Preparation method and application of nano-drug carrier with long circularity

Examples

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preparation example Construction

[0049] In the preparation method of the present invention, at first the chitosan is surface-modified with polyethylene glycol, and then the electrostatic interaction between temperature, pH-sensitive anionic polymer and the modified chitosan is utilized under mild conditions, The molecular chains are intertwined by polyelectrolyte composite method to form nanoparticles with uniform particle size. Macromolecular complexes synthesized by polyelectrolyte complexes have many similarities with biological macromolecules in terms of structure and performance, such as surface charge, hydrophilicity and hydrophobicity, and selective transport of small molecules, which help to simulate the process in vivo and realize Some special functions have great application prospects in the field of biomedicine.

[0050] figure 1 For the NMR spectrum of the grafted product CS-g-mPEG prepared by the inventive method, the 3.58ppm place is the H(d) peak in the -NHCH2(e)CH2(d)-, and the 3.48ppm place ...

Embodiment 1

[0057] A kind of preparation method of the present invention has long circulation nano-drug carrier, specifically implements according to the following steps:

[0058] Step 1, adopt one-step method to prepare polyethylene glycol modified chitosan CS-g-mPEG, at first, formaldehyde and the amino group on chitosan form Schiffer's base, then the hydroxyl group on polyethylene glycol monomethyl ether and Schiffer's base Addition reaction of Freund's base produces polyethylene glycol monomethyl ether grafted chitosan;

[0059] Specifically: Dissolve chitosan (CS) in formic acid (HCOOH), after it is completely dissolved, add dimethyl sulfoxide (DMSO) to dilute, then add polyethylene glycol monomethyl ether (mPEG), and continue stirring 15min, finally add formaldehyde (HCHO) solution with a mass fraction of 37%, continue to react for 4h, after stopping the reaction, move the reaction solution to a dialysis bag, dialyze with deionized water for 3 days, then move to a centrifuge tube, a...

Embodiment 2

[0073] A kind of preparation method of the present invention has long circulation nano-drug carrier, specifically implements according to the following steps:

[0074] Step 1, adopt one-step method to prepare polyethylene glycol modified chitosan CS-g-mPEG, at first, formaldehyde and the amino group on chitosan form Schiffer's base, then the hydroxyl group on polyethylene glycol monomethyl ether and Schiffer's base Addition reaction of Freund's base produces polyethylene glycol monomethyl ether grafted chitosan;

[0075] Specifically: Dissolve chitosan (CS) in formic acid (HCOOH), after it is completely dissolved, add dimethyl sulfoxide (DMSO) to dilute, then add polyethylene glycol monomethyl ether (mPEG), and continue stirring 15min, finally add the formaldehyde (HCHO) solution that the mass fraction is 37%, continue to react for 4.5h, after stopping the reaction, move the reaction solution to the dialysis bag, dialyze with deionized water for 3 days, then move to the centri...

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Abstract

The invention discloses a preparation method of a nano-drug carrier with long circularity, which specifically comprises the following steps: firstly, forming Schiff's base by formaldehyde and amino on chitosan, and then carrying out addition reaction on hydroxyl on methoxypolyethylene glycol and the Schiff's base to generate methoxypolyethylene glycol grafted chitosan; carrying out free radical polymerization on NIPAm and AMPS to prepare a polyanion PNAM; taking CS-g-mPEG as a polycation, taking PNAM as a polyanion, and preparing the long-cycle nano-drug carrier through a polyelectrolyte composite method. The nano-drug carrier prepared by the invention not only has the advantages of biodegradability, no toxicity, low immunogenicity, bacteriostasis, cancer resistance and the like of chitosan, but also has good biocompatibility and long circularity in blood of polyethylene glycol, so that the selectivity of small-molecule chemotherapeutic drugs to cancer cells is improved, the medication frequency is reduced, the damage to normal tissues and cells is reduced, and the bioavailability of the medicine is improved.

Description

technical field [0001] The invention belongs to the technical field of preparation of biomedical polymer materials, and in particular relates to a preparation method of a long-circulating nano-medicine carrier, and also relates to an application of the long-circulating nano-medicine carrier. Background technique [0002] Chemotherapy drugs widely used in clinical practice are widely distributed in the body, especially in some normal tissues, which not only reduces the bioavailability of drugs, but also causes significant toxic and side effects on normal tissues. In addition, the circulation time of the drug in the blood is too short, so it is difficult to reach the lesion site. Improving the selectivity of chemotherapeutic drugs to cancer cells, reducing their distribution in non-targeted sites, and improving drug utilization are the keys to improving the efficacy of cancer therapeutic drugs. [0003] Chitosan is an abundant natural cationic polymer with unique properties s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K31/722A61K45/00A61K47/32A61P31/04A61P35/00B82Y5/00B82Y30/00B82Y40/00C08G81/00C08F220/58C08F220/54
CPCA61K9/5161A61K47/32A61K45/00B82Y5/00B82Y30/00B82Y40/00A61K31/722A61P35/00A61P31/04C08G81/00C08F220/585C08F220/54
Inventor 赵婧邓星月潘桂旭丁涛吴超
Owner XI'AN POLYTECHNIC UNIVERSITY
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