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Preparation method for polyamide based polyelectrolyte nano-micelle

A polyelectrolyte and nano-micelle technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of high toxicity and side effects of doxorubicin, and achieve simple steps and excellent results. Drug loading and controlled release effects, effects of avoiding synthetic steps

Active Publication Date: 2015-06-10
AFFILIATED HOSPITAL OF NANTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the side effects of doxorubicin are also very large

Method used

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  • Preparation method for polyamide based polyelectrolyte nano-micelle
  • Preparation method for polyamide based polyelectrolyte nano-micelle
  • Preparation method for polyamide based polyelectrolyte nano-micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of amide bond-containing polyelectrolyte terpolymer: mix 1.5g L-glutamic acid and 4gmPEG evenly, add 0.02g stannous chloride dihydrate as catalyst, prepolymerize at 110°C for 3h, raise temperature to 130°C, and maintain vacuum at 0.085 Mpa, stop heating after reacting for 8 hours, dissolve the product with ethanol, filter to remove unreacted glutamic acid, distill the filtrate under reduced pressure at 50°C, dissolve the product with chloroform, and precipitate with anhydrous ether to obtain a light yellow viscous liquid, fully Dry and set aside.

[0021] Preparation of drug-loaded micelles: The drug-loaded micelles were prepared by polyion complex method. Dissolve 0.2g of PGlu-co-PLA-co-mPEGG (LP105-DOX) in 20g of water, stir magnetically until the copolymer is completely dissolved, and gradually add aqueous solution of doxorubicin until the solution turns red and has obvious Tyndall phenomenon Stopped at 1 hour, then continued to stir for 24 hours to stabil...

Embodiment 2

[0024] The molar ratio of Glu, LA and mPEG is 1:0.5:0.5, and other synthesis processes are the same as in Example 1.

Embodiment 3

[0026] The molar ratio of Glu, LA and mPEG is 1:1:0.5, and other synthesis processes are the same as in Example 1.

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Abstract

Belonging to the technical field of carriers and sustained-release materials, the invention discloses a preparation method for a polyelectrolyte composite nano-micelle as a drug carrier. The method provided by the invention takes glutamic acid (Glu), lactic acid (LA) and mPEG as the raw materials to carry out direct copolycondensation reaction so as to obtain an amido bond containing polyelectrolyte terpolymer, and the terpolymer and adriamycin are compounded in a water solution to form adriamycin. As the main chain of the polyelectrolyte copolymer contains a polyamide chain segment structure and a polyester chain segment structure at the same time, the degradability in water is slowed down, the polymer stability is improved, and by compounding the copolymer with the anticancer drug adriamycin, the obtained nano-micelle has strengthened stability, and can be expected to improve the drug bioavailability. Drug release is controlled by pH value and ionic strength. The nano-micelle provided by the invention has the characteristics of simple synthesis, good micelle stability, no tedious synthesis step, no use of any organic solvent, no toxicity and environmental protection, and has application prospects.

Description

technical field [0001] The invention relates to a preparation method of biodegradable nano-micelle based on polyamide polyelectrolyte, and belongs to the technical field of carriers and slow-release materials. Background technique [0002] Polyelectrolyte complex micelles are formed by electrostatic interaction of two oppositely charged components. One of the outstanding advantages of this type of micelles is that they can be loaded with charged drugs, genes or enzymes, and the preparation conditions are mild and simple. Researchers use the characteristics that polyelectrolyte complexes can directly or indirectly participate in some complex life activities in the living body, and are used in the fields of stimuli-responsive drug controlled release, cell immune isolation and transplantation, polypeptide protein drug controlled release, gene therapy and artificial vaccines. Intensive studies have been conducted and significant progress has been made, which is of great signific...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/107A61K31/704A61P35/00
Inventor 倪才华张亚南王洁李旺张猛
Owner AFFILIATED HOSPITAL OF NANTONG UNIV