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Polymer micelle medicine carrying system using amino acid as stabilizing agent

A technology of polymer glue and amino acid, which can be used in cardiovascular system diseases, antipyretics, anti-inflammatory agents, etc., and can solve problems that have not been seen before

Inactive Publication Date: 2012-11-07
FANTAI INST OF CHEM MEDICINES NANJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Experiments have found that amino acids can improve the physical stability of drug-loaded micelles, but no related research has been reported so far

Method used

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  • Polymer micelle medicine carrying system using amino acid as stabilizing agent
  • Polymer micelle medicine carrying system using amino acid as stabilizing agent
  • Polymer micelle medicine carrying system using amino acid as stabilizing agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Synthesis of amphiphilic block copolymer mPEG-PDLLA

[0074] Weigh 16 g of methyl polyethylene glycol and 24 g of lactide, place them in a closed reactor, add 50 mg of stannous octoate, and heat up to 120-140°C under nitrogen flow to melt the solid, and raise the temperature to 150-180 React at °C for 6 hours. After cooling, a white solid crude product was obtained. After the crude product is dissolved in 1ml of dichloromethane, it is added to 100ml of ether under stirring, filtered, washed with ether three times, and the product is dried under vacuum for 24 hours.

[0075] The NMR (D-chloroform as solvent) spectrum of the product confirmed the mass ratio and molecular weight of methyl polyethylene glycol to polylactic acid in the polymer with the peak area ratio of 5.2 ppm (PLA) and 3.6 ppm (PEG).

Embodiment 2

[0076] Example 2 Preparation of docetaxel polymer micelles

[0077] Pipette 10ml 50mg / ml polymer acetonitrile solution into the eggplant-shaped bottle, add 10ml 5mg / ml docetaxel acetonitrile solution, place the eggplant-shaped bottle on the rotary evaporator, reduce pressure (-0.1MPa), and water bath temperature 50 ℃, rotating speed 20 rpm, rotary evaporation for 30 minutes, add 50ml of 0.2mg / ml arginine aqueous solution and spin for 1 minute, remove the eggplant-shaped bottle, vortex on the vortexer for 1 minute, the resulting solution is filtered through 0.22μm Membrane filtration, take the filtrate into a 10ml vial, 2ml per bottle, immediately freeze-dry to obtain a white solid.

Embodiment 3

[0078] Example 3 Preparation and stability investigation of paclitaxel polymer micelles

[0079] Pipette 6ml 50mg / ml polymer acetonitrile solution into the eggplant-shaped bottle, add 6ml 10mg / ml paclitaxel acetonitrile solution, place the eggplant-shaped bottle on the rotary evaporator, reduce pressure (-0.1MPa), water bath temperature 50℃, rotation speed 20 rpm, rotary evaporation for 30 minutes, add 25ml of 0.2mg / ml aspartic acid aqueous solution and spin for 1 minute, remove the eggplant-shaped bottle, vortex on a vortexer for 1 minute, and filter the resulting solution through a 0.22μm filter membrane , Packed in 10ml vials, 2.5ml per bottle, immediately freeze-dried to obtain a white solid. The solids are mixed with 0.9% sodium chloride injection or 5 ml 5% glucose injection to prepare a clear transparent slightly blue opalescent paclitaxel polymer micelle solution. The resulting micellar solution was kept at 25 degrees Celsius for 24 hours. The results of visual inspectio...

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Abstract

The invention relates to a polymer micelle medicine carrying system using an amino acid as a stabilizing agent and a preparation method thereof, wherein the medicine carrying system can be used as a medicament carrier composition, and the medicament carrier composition comprises an amphipathic segmented copolymer and amino acid, wherein the amphipathic segmented copolymer comprises a diblock copolymer and a triblock copolymer, the amino acid is selected from 20 kinds of common amino acid, and the mixture ratio (w / w) of the amphipathic segmented copolymer to the amino acid is 100 / 0.01-1.00 / 99.99.

Description

Technical field: [0001] The invention relates to a polymer micelle drug-carrying system using amino acid as a stabilizer and its preparation. Background technique: [0002] Polymer micelles are a drug delivery system for poorly soluble drugs developed in recent years. They are composed of amphiphilic block polymers, have low critical micelle concentration (CMC) (<100□g / ml), and have core- Shell-like structure, where the core is the hydrophobic part and the shell is the hydrophilic part. Polymer micelles can wrap poorly soluble drugs in the core to solubilize poorly soluble drugs. Drug-loading polymer micelles often choose biodegradable amphiphilic polymers as materials. This type of amphiphilic polymers can be diblock AB type or triblock ABA, BAB type. For their structure, see Torchilin. , VP, Structure and design of polymeric surfactant-based drug delivery systems. JControl Release, 2001.73(2-3): p.137-72. Block copolymers have lower critical micelle concentration (CMC) and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/34A61P3/10A61P9/00A61P29/00A61P31/00A61P35/00
CPCA61K47/183A61K9/1075A61K47/20A61P3/10A61P9/00A61P29/00A61P31/00A61P35/00
Inventor 吴建梅
Owner FANTAI INST OF CHEM MEDICINES NANJING
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