Synthesis method of PLGA (poly(lactic-co-glycolic acid)) chemically modified material and method for preparing nanoparticles from material

A glycolic acid copolymer chemistry and glycolic acid copolymer technology, applied in the field of synthesis of polylactic acid-glycolic acid copolymer chemically modified materials, to achieve uniform particle size distribution, stable properties, smooth and complete surface

Active Publication Date: 2016-10-26
西安俊航网络科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Currently, there is no information on the use of gallic acid derivatives (C 26 h 21 f 6 N 3 o 4 ) is chemically bonded to PLGA, enabling it to specifically recognize and bind HDACs

Method used

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  • Synthesis method of PLGA (poly(lactic-co-glycolic acid)) chemically modified material and method for preparing nanoparticles from material
  • Synthesis method of PLGA (poly(lactic-co-glycolic acid)) chemically modified material and method for preparing nanoparticles from material
  • Synthesis method of PLGA (poly(lactic-co-glycolic acid)) chemically modified material and method for preparing nanoparticles from material

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Synthesis of polylactic acid-glycolic acid copolymer chemically modified material modified by embodiment 1 gallic acid derivative

[0025] Dissolve 200mg of poly(lactic-co-glycolic acid) (PLGA) completely in 10mL of dichloromethane, stir in ice bath for 20min until uniform, then add 2.3mg of N-hydroxysuccinimide, 500μL of triethyl Amine and 3.8 mg of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride were gradually heated to room temperature for 10 hours. Take the gallic acid derivative (C 26 h 21 f 6 N 3 o 4 , whose structure is as figure 1 shown), which was dissolved in 1 mL of dichloromethane to obtain a dichloromethane solution of gallic acid derivatives. Add the dichloromethane solution of gallic acid derivatives dropwise to the above reaction system, and continue to react for 20 hours at room temperature. Washing with an aqueous solution, drying overnight with anhydrous sodium sulfate, and then filtering, removing the solvent from the filtrate und...

Embodiment 2

[0029] The preparation of embodiment 2 nanoparticles

[0030] Dissolve 60 mg of the gallic acid derivative-modified polylactic-co-glycolic acid copolymer chemical modification material prepared in Example 1 in 3 mL of dichloromethane, and add it to 15 mL of a 1% polyvinyl alcohol aqueous solution, Mix evenly to obtain a mixed solution, process the mixed solution with a probe-type ultrasonic instrument for 5 minutes to form a nanoemulsion (ultrasonic power is 800W), then magnetically stir for 4 hours, remove the organic solvent in the nanoemulsion, make it completely solidified to form nanoparticles, After 10min (10000r / min) high-speed centrifugation, washing and drying, the nanoparticle with the polylactic acid-glycolic acid copolymer modified by the gallic acid derivative as the carrier is obtained.

[0031] The morphology of the nanoparticles was observed under a scanning electron microscope, such as image 3 As shown, it can be seen that the surface of the nanoparticles is...

Embodiment 3

[0032] Synthesis of polylactic acid-glycolic acid copolymer chemically modified material modified by embodiment 3 gallic acid derivatives

[0033] Dissolve 200mg of poly(lactic-co-glycolic acid) (PLGA) completely in 10mL of dichloromethane, stir in ice bath for 20min until uniform, then add 2.3mg of N-hydroxysuccinimide, 500μL of triethyl Amine and 3.8 mg of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride were gradually heated to room temperature for 11 hours. Take the gallic acid derivative (C 26 h 21 f 6 N 3 o 4 , whose structure is as figure 1 shown), which was dissolved in 1 mL of dichloromethane to obtain a dichloromethane solution of gallic acid derivatives. Add the dichloromethane solution of gallic acid derivatives dropwise to the above reaction system, and continue to react for 24 hours at room temperature. Washing with an aqueous solution, drying overnight with anhydrous sodium sulfate, and then filtering, removing the solvent from the filtrate un...

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Abstract

The invention provides a synthesis method of a PLGA (poly(lactic-co-glycolic acid)) chemically modified material and a method for preparing nanoparticles from the material. PLGA reacts with a gallic acid derivative, an amino group on a gallic acid derivative molecule and a carboxyl group on PLGA are subjected to a condensation reaction to form an amido bond, and PLGA is structurally modified, so that PLGA can specifically recognize and combine HDACs (histone deacetylases). Then the nanoparticles are prepared from gallic acid derivative-modified PLGA through ultrasonic treatment, can be specifically combined with the HDACs, have smooth and complete surfaces, are large in entrapment capability, uniform in particle size distribution, stable in property and capable of realizing directional delivery of carried drugs and have the bright application prospect.

Description

technical field [0001] The invention belongs to the technical field of nanometer materials, and relates to a method for synthesizing a polylactic acid-glycolic acid copolymer chemically modified material and a method for preparing nanoparticles with the material. Background technique [0002] Polylactic acid-glycolic acid copolymer (PLGA) is a polymer material polymerized by lactic acid and glycolic acid according to a certain ratio, and its degradation products are lactic acid and glycolic acid, which are also human metabolites. Due to its good biocompatibility and biodegradability, stable quality, and adjustable degradation rate, it has been widely used as the skeleton material of micro-nano controlled release systems in recent years. [0003] Since PLGA is a synthetic lipophilic polymer material, there are certain limitations in application, especially the lack of specific binding to body cells, so it is difficult for the micro-nano controlled release system prepared by P...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/91C08J3/12A61K47/48A61K31/192A61P35/00
CPCA61K31/192C08G63/912C08J3/12C08J2367/04
Inventor 卢闻张杰贺浪冲师亚玲邵晓玮杨晓莹潘成成
Owner 西安俊航网络科技有限公司
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