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Method for preparing charge-driven self-assembled chitosan-based drug-loaded nanoparticles

A drug-loaded nano and chitosan technology, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations containing active ingredients. Toxicity and other issues, achieve good biocompatibility and biomedical prospects, reduce the risk of solvent residues, and controllable size and potential

Active Publication Date: 2018-06-29
WENZHOU MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Glutaraldehyde has high biological toxicity and is likely to bring health risks, so it is not suitable for a large number of applications in biomaterials
Although genipin is considered to be a relatively safe cross-linking, a large amount of residues is likely to bring health risks

Method used

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  • Method for preparing charge-driven self-assembled chitosan-based drug-loaded nanoparticles
  • Method for preparing charge-driven self-assembled chitosan-based drug-loaded nanoparticles
  • Method for preparing charge-driven self-assembled chitosan-based drug-loaded nanoparticles

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Embodiment 1

[0043] Embodiments of the present invention include the following steps:

[0044] (1) Preparation of PEG-PGA amphoteric dissociation copolymer:

[0045]Benzyl glutamate-N-carbonyl intracyclic anhydride induced by amino PEG to form a block copolymer of PEG and polybenzyl glutamate, which was hydrolyzed under basic conditions to remove polybenzyl glutamate The terminal benzyl group forms a block copolymer of PEG-PGA. The synthesis example is as follows: 1.2 g of benzyl glutamate-N-carbonyl ring anhydride was dissolved in 20 mL of dry nitrogen nitrogen dimethylformamide, mixed with amino PEG and reacted at 38 degrees for 48 hours under nitrogen protection. The block copolymer of PEG and polybenzyl glutamate was obtained by dialysis, and the benzyl group was removed under the action of NaOH to form a PEG-PGA block copolymer. see figure 2 As stated, it can be confirmed that the PEG-PGA block copolymer has been successfully synthesized, and its molecular structural formula is: ...

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Abstract

The invention discloses a method for preparing charge-driven self-assembled chitosan-based drug-loaded nanoparticles. The method comprises the following steps: (1) forming a PEG and benzyl polyglutamic acid block copolymer by PEG amino-induced benzyl glutamate-N-carbonyl cyclic anhydride, hydrolyzing the block copolymer under alkaline conditions to remove a benzyl at the benzyl polyglutamic acid end to form a PEG-PGA block copolymer; (2) preparing a chitosan-based doxorubicin prodrug; (4) preparing charge-driven self-assembled nanoparticles. The materials selected for the strategy for preparing the doxorubicin-based chitosan-based nanoparticles are PEG and PGA materials which are generally proved to have better biocompatibility, and the strategy for forming chitosan nanoparticles has better biocompatibility and biomedical prospects.

Description

technical field [0001] The invention belongs to the field of preparation of functional materials, in particular to a preparation method of charge-driven self-assembled chitosan-based drug-loaded nanoparticles. Background technique [0002] Chitosan (CS) is a kind of natural polymer polysaccharide with punctuality, which has the characteristics of non-toxic, degradable, good biocompatibility and low immunogenicity, and can be used as a biomedical material. Due to its positive nature, it can be used as a delivery material for negatively charged DNA, RNA, and other biomacromolecules. Studies have also pointed out that chitosan has a similar function to targeting CD44 (highly expressed factor in tumor tissue) as hyaluronic acid. In addition, unlike many nanoparticles, chitosan-modified nanoparticles are mainly distributed in the nucleus after endocytosis, which is more conducive to the delivery of antitumor drugs. Because most anti-tumor drugs (such as doxorubicin, paclitaxel,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/36A61K47/42A61K9/16A61K31/704A61P35/00
CPCA61K9/1641A61K9/1652A61K9/1658A61K31/704
Inventor 林森南开辉罗梦梦王冬梅
Owner WENZHOU MEDICAL UNIV
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