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Polyglycerol fatty acid ester derivative containing polysialic acid group as well as synthesis method and application of polyglycerol fatty acid ester derivative in pharmaceutical preparations

A technology of polysialic acid and fatty acid ester, applied in the field of medicine, can solve problems such as decreased activity, achieve the effects of good biocompatibility and biodegradability, good clinical transformation and industrial development prospects

Active Publication Date: 2021-01-05
SHAOXING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have pointed out that PSA-asparaginase has no immunogenicity, and the activity of asparaginase is hardly affected, but the activity is severely reduced after PEG modification

Method used

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  • Polyglycerol fatty acid ester derivative containing polysialic acid group as well as synthesis method and application of polyglycerol fatty acid ester derivative in pharmaceutical preparations
  • Polyglycerol fatty acid ester derivative containing polysialic acid group as well as synthesis method and application of polyglycerol fatty acid ester derivative in pharmaceutical preparations
  • Polyglycerol fatty acid ester derivative containing polysialic acid group as well as synthesis method and application of polyglycerol fatty acid ester derivative in pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The synthesis of embodiment 1 polysialic acid-ten polyglycerol distearate

[0036] PSA-PG preparation process of the present invention: at first, feed ratio is polysialic acid (PSA) / decaglyceryl distearate (PG 10 -2C 18 ) / N-hydroxysuccinimide (NHS) / 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) / triethylamine (TEA)=1: 1:2:4:4 (molar ratio); Dissolve an appropriate amount of PSA in 5mL of formamide (FA), add EDC / NHS in proportion, activate at 4°C for 90min, the system is clear at this time; then dissolve in 2mL of FA PG in 10 -2C 18 Add to the reaction system, add TEA, stir at room temperature for 48h, the reaction solution is clear; then transfer the reaction solution to a dialysis bag (molecular weight cut-off 10kDa), the dialysis medium is concentrated hydrochloric acid-water (V / V, 1:100) system, The volume of dialysis was 1000mL, and the dialysis medium was changed every 4 hours for a total of 24 hours of dialysis; finally, part of the water was r...

Embodiment 2

[0044] The synthesis of embodiment 2 polysialic acid-dodepolyglycerol dipalmitate

[0045] The PSA-PG preparation process of the present invention: at first, feed ratio is polysialic acid (PSA) / dodecyl glyceryl dipalmitate (PG 12 -2C 16 ) / N-hydroxysuccinimide (NHS) / 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) / triethylamine (TEA)=1: 1:2:4:4 (molar ratio); Dissolve an appropriate amount of PSA in 5mL of formamide (FA), add EDC / NHS in proportion, activate at 4°C for 90min, the system is clear at this time; then dissolve in 2mL of FA PG in 12 -2C 16 Add to the reaction system, add TEA, stir at room temperature for 48h, the reaction solution is clear; then transfer the reaction solution to a dialysis bag (molecular weight cut-off 10kDa), the dialysis medium is concentrated hydrochloric acid-water (V / V, 1:100) system, The volume of dialysis is 1000mL, and the dialysis medium is changed every 4 hours for a total of 24 hours of dialysis; finally, part of the wat...

Embodiment 3

[0053] The synthesis of embodiment 3 polysialic acid-hexapolyglyceryl laurate

[0054] PSA-PG preparation process of the present invention: at first, feed ratio is polysialic acid (PSA) / hexapolyglycerol laurate (PG 6 -C 12 ) / N-hydroxysuccinimide (NHS) / 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) / triethylamine (TEA)=1: 1:2:4:4 (molar ratio); Dissolve an appropriate amount of PSA in 5mL of formamide (FA), add EDC / NHS in proportion, activate at 4°C for 90min, the system is clear at this time; then dissolve in 2mL of FA PG in 6 -C 12 Add to the reaction system, add TEA, stir at room temperature for 48h, the reaction solution is clear; then transfer the reaction solution to a dialysis bag (molecular weight cut-off 10kDa), the dialysis medium is concentrated hydrochloric acid-water (V / V, 1:100) system, The dialysis volume is 1000mL, and the dialysis medium is changed every 4 hours for a total of 24 hours of dialysis; finally, part of the water is removed by ro...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a polyglycerol fatty acid ester derivative (PSAPG) containing a polysialic acid group as well as a synthesis method and application of the polyglycerol fatty acid ester derivative (PSAPG) in a medicinal preparation, in particular to preparation and modification of a particle preparation. The structural formula of the PSA-PG is shown as the specification, wherein the PSA represents a polysialic acid group, PG represents a polyglycerol fatty acid ester fragment, X represents the number of PG fragments graftedin a PSA molecule, (X + Y) represents the number of sialic acid units in the PSA molecule, n represents the polymerization degree of polyglycerol in the PG fragment, m represents the number of carbonatoms of a hydrocarbon chain in the PG fragment, 1 < = X < = 80, and 2 < = X + Y < = 200,X / (X + Y) is 0.5%-80%, n is greater than or equal to 1 and less than or equal to 100, and m is greater than orequal to 4 and less than or equal to 32. The particle preparation modified or prepared by the PSA-PG has high physicochemical stability, low immunogenicity, long in-vivo circulation and high tumor targeting.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to a polyglycerol fatty acid ester derivative containing a polysialic acid group, its synthesis method and its application in pharmaceutical preparations, especially for the preparation and modification of microparticle preparations. Background technique [0002] All disease is a process, not a state, in which the immune system is always involved. After the organic combination of immunology and pharmacy, we can transform the strategy of avoiding immune recognition into using the immune system for drug delivery system (Drug delivery system, DDS) design to achieve efficient targeting. Therefore, in the future drug delivery system (DDS), the key links involved in nanotechnology actively "find" immune cells, improve the immune environment, and rely on a strong immune system to cure diseases. [0003] Classical immunology theory points out that the percentages of various whi...

Claims

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Application Information

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IPC IPC(8): C08B37/00C08G81/00A61K47/34A61K47/36A61K31/337A61K31/704A61K31/05A61K31/12A61P35/00A61K8/85A61K8/73A61Q19/00
CPCC08B37/0006C08G81/00A61K47/34A61K47/36A61K31/337A61K31/704A61K31/05A61K31/12A61P35/00A61K8/85A61K8/73A61Q19/00A61K2800/524
Inventor 骆翔沈琳暄熊婷婷徐歌赵礼普汪泽卿邓莉萍朱柯武虞国棋沈润溥
Owner SHAOXING UNIVERSITY
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