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Terminal amido group start-type poly (lactic-co-glycolic acid)/polyglycol block copolymer, preparation method, medicament-carried nano micelle and application

A polyglycolide and block copolymer technology, which can be applied in the directions of ether/acetal active ingredients, antitumor drugs, drug combinations, etc., can solve the problem of less modifiable end groups and low drug encapsulation efficiency. and other problems, to achieve the effect of inhibiting tumor angiogenesis and improving the inhibition rate

Inactive Publication Date: 2008-02-20
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used polyethylene glycol (PEG) / polyethylene lactide (PLGA) block copolymers are linear copolymers, but linear copolymers have fewer modifiable end groups, which are useful for the encapsulation of drugs low rate

Method used

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  • Terminal amido group start-type poly (lactic-co-glycolic acid)/polyglycol block copolymer, preparation method, medicament-carried nano micelle and application
  • Terminal amido group start-type poly (lactic-co-glycolic acid)/polyglycol block copolymer, preparation method, medicament-carried nano micelle and application
  • Terminal amido group start-type poly (lactic-co-glycolic acid)/polyglycol block copolymer, preparation method, medicament-carried nano micelle and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] A kind of amine-terminated star polylactide / polyethylene glycol block copolymer is made by following method:

[0047] (1) Add glycolide and lactide with a molar ratio of 1:5 to the polymerization sealed tube, and then add polyamide-amine-OH with a molar ratio of 1:50 to the monomer Dendritic macromolecule constitutes reactant, adds stannous octoate as catalyst, and the addition mass of described catalyst is 0.1% of described reactant mass, vacuumizes nitrogen replacement 3 times, is 40Pa sealing tube at vacuum degree, at 135 ℃, React for 48 hours to obtain hydroxyl-terminated star polylactide;

[0048] (2) The hydroxyl-terminated star-shaped polyglycolide and succinic anhydride are prepared according to the molar ratio of the hydroxyl group in the hydroxyl-terminated star-shaped polyglycolide molecule to succinic anhydride of 1:14, at 25°C , and reacted for 30 hours to obtain carboxyl-terminated star polylactide;

[0049] (3) According to the mass ratio of 1:20, the c...

Embodiment 2

[0054] A kind of amine-terminated star polylactide / polyethylene glycol block copolymer is made by following method:

[0055] (1) Add glycolide and lactide with a molar ratio of 1:1 to the polymerization sealed tube, then add inositol with a molar ratio of 1:30 to form the reactant, add Stannous octoate is the catalyst, the added mass of the catalyst is 0.1% of the mass of the reactant, evacuated and replaced by nitrogen twice, sealed at a vacuum of 80Pa, and reacted for 60 hours at 110°C to obtain a star-shaped hydroxyl group. Polyethylene lactide;

[0056] (2) The hydroxyl-terminated star polylactide and succinic anhydride are prepared at 20° C. according to the molar ratio of the hydroxyl group in the hydroxyl-terminated star polylactide molecule to succinic anhydride of 1:15. , and reacted for 40 hours to obtain carboxyl-terminated star polylactide;

[0057] (3) According to the mass ratio of 1:10, the carboxyl-terminated star polylactide is dissolved in anhydrous toluene...

Embodiment 3

[0059] A kind of amine-terminated star polylactide / polyethylene glycol block copolymer is made by following method:

[0060] (1) Add glycolide and lactide with a molar ratio of 1:10 to the polymerization sealed tube, and then add glycerol with a molar ratio of 1:100 to form the reactant, Add stannous octoate as a catalyst, the mass of the catalyst added is 0.1% of the mass of the reactant, evacuate nitrogen for 4 times, seal the tube at a vacuum degree of 5Pa, and react at 150°C for 24 hours to obtain the hydroxyl-terminated star Type polyethylene lactide;

[0061] (2) The hydroxyl-terminated star-shaped polyglycolide and succinic anhydride are prepared according to the molar ratio of the hydroxyl group in the hydroxyl-terminated star-shaped polyglycolide molecule to succinic anhydride as 1:9, at 30°C , and reacted for 20 hours to obtain carboxyl-terminated star polylactide;

[0062] (3) According to the mass ratio of 1:30, the carboxyl-terminated star polylactide is dissolv...

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Abstract

The invention discloses a terminal amidocyanogen star-shaped lactic and glycolic acid / polyethyleneglycol segmented copolymer, a preparation method, drug-loaded nano-micelle and application thereof. The preparation method of the terminal amidocyanogen star-shaped lactic and glycolic acid / polyethyleneglycol segmented copolymer: (1) glycolide, polyhydroxy activator, stannous octoate and lactide are added into a polymerized tube sealing for vacuumized nitrogen permutation and reaction, and terminal hydroxyl star-shaped lactic and glycolic acid can be obtained; (2) butanedioic anhydride is added for reaction to prepare terminal carboxyl group star-shapedl actic and glycolic acid; (3) the terminal carboxyl group star-shaped lactic and glycolic acid is dissolved in anhydrous toluene, then doublepointed amidocyanogen polyethyleneglycol, N and N'- dicyclohexylcarbodiimide are added for reaction, solvent is evaporated to dryness and aether is added for sedimentation to prepare the terminal amidocyanogen star-shaped lactic and glycolic acid / polyethyleneglycol segmented copolymer which can form about 100nm of micelle automatically in water solution. Hydrophobic nature drugs can be loaded in the caryon of the micelle and putamen surface of the micelle is rich of high activity and freedom terminal amidocyanogen arms that can couple with various bioactivators to achieve the effect of targeted release.

Description

technical field [0001] The invention relates to a polyethylene lactide / polyethylene glycol block copolymer, a preparation method of the copolymer, drug-loaded nano micelles and applications. Background technique [0002] In recent years, self-assembled systems formed by amphiphilic polymers have attracted widespread attention and research interest due to their potential application prospects in the fields of catalysts, drug controlled release systems, microreactors, and self-assembled materials. Among them, the research on using amphiphilic block copolymer micelles as drug carriers is still one of the current hotspots. By adjusting the length of the hydrophilic / hydrophobic segment and self-assembly conditions in the copolymer, micelles with a diameter of about 10-100 nm can be obtained. When used as a drug carrier for systemic administration, such small-sized polymer micelles with a hydrophilic shell can effectively reduce or avoid rapid renal clearance and the chance of be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08G63/91C08G63/08A61K47/34A61K9/00A61K31/09A61K31/337A61K31/704A61K38/08A61P35/00
Inventor 王亮宋存先
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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