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A polylactic acid-glycolic acid copolymer nano drug carrier and its preparation method and application

A technology of glycolic acid copolymer and glycolic acid, which is applied in the direction of nano-medicine, nanotechnology, nanotechnology, etc., can solve the problems of poor drug absorption, weak cell uptake ability, and lack of specific binding, etc., to achieve enhanced drug Therapeutic effect, enhancement of cell uptake ability, effect of uptake ability enhancement

Active Publication Date: 2017-08-01
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PLGA also has the following disadvantages as a drug carrier material: (1) PLGA microspheres lack specific binding to body cells, the cell uptake ability is not strong, and the drug absorption effect is not good; (2) PLGA drug-loaded microspheres have a negative effect on drug release. Non-selective, that is, drug release cannot be concentrated in the tumor tissue or tumor cells, making the drug utilization rate low and easy to cause damage to normal tissues
Its defect is that this invention is mainly used for encapsulating hydrophilic drugs, and the drugs for treating cancer are mostly hydrophobic; in addition, the PLGA microspheres modified by chitosan have disadvantages such as poor stability.

Method used

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  • A polylactic acid-glycolic acid copolymer nano drug carrier and its preparation method and application
  • A polylactic acid-glycolic acid copolymer nano drug carrier and its preparation method and application
  • A polylactic acid-glycolic acid copolymer nano drug carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] PLGA was dissolved in a mixed solvent of dichloromethane and ethanol with a volume ratio of 3:1 to prepare a PLGA solution with a concentration of 20 mg / mL. The above PLGA solution was dropped dropwise into 0.75% PVA aqueous solution under the condition of vortex oscillation, and was ultrasonically emulsified with an ultrasonic cell pulverizer for 60 s under the condition of ultrasonic power of 12 W, and then an equal volume of the above The PVA aqueous solution was added to the emulsion, and the organic solvent was removed by continuous stirring for 3 h, so that the nanospheres were solidified and formed, centrifuged at 4 °C and 13000 rpm for 10 min, and washed twice to obtain the product P. Aqueous acetic acid was used as a solvent to prepare chitosan solutions with concentration gradients of 1.25 mg / mL, 2.5 mg / mL and 3.75 mg / mL and adjust the pH to 6.0. Disperse the collected microspheres in the above chitosan solutions of different concentrations, stir for 3 h to ma...

Embodiment 2

[0053] Dissolving PLGA in a mixed solvent of dichloromethane and ethanol with a volume ratio of 3:1 is made into a PLGA solution with a concentration of 20 mg / mL; the chitosan aqueous solution with a concentration of 3.75 mg / mL is prepared and the pH value is adjusted to 6.0. The above PLGA solution was dropped dropwise into 0.75% PVA aqueous solution under the condition of vortex oscillation, and was ultrasonically emulsified with an ultrasonic cell pulverizer for 60 s under the condition of ultrasonic power of 12 W, and then an equal volume of the above The PVA aqueous solution was added to the emulsion, and the organic solvent was removed by continuous stirring for 3 h, so that the nanospheres were solidified and formed, centrifuged at 4 °C and 13000 rpm for 10 min, and washed twice to obtain the product P. The collected microspheres were dispersed in the above-mentioned chitosan aqueous solution, stirred continuously for 3 h to make chitosan adsorb on the PLGA microspheres...

Embodiment 3

[0056] PLGA was dissolved in a mixed solvent of dichloromethane and ethanol with a volume ratio of 3:1 to prepare a PLGA solution with a concentration of 20 mg / mL. A chitosan aqueous solution with a concentration of 3.75 mg / mL was prepared and the pH value was adjusted to 6.0. The above PLGA solution was dropped dropwise into 0.75% PVA aqueous solution under the condition of vortex oscillation, and was ultrasonically emulsified with an ultrasonic cell pulverizer for 60 s under the condition of ultrasonic power of 12 W, and then an equal volume of the above The PVA aqueous solution was added to the emulsion, and the organic solvent was removed by continuous stirring for 3 h, so that the nanospheres were solidified and formed, centrifuged at 4 °C and 13000 rpm for 10 min, and washed twice to obtain the product P. Disperse the collected microspheres in the above chitosan aqueous solution, stir continuously for 3 h to make chitosan adsorb on the PLGA microspheres, centrifuge at 4 ...

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Abstract

The invention provides a PLGA (polylactic acid-hydroxyacetic acid) nano-drug carrier which is composed of PLGA nano microsphere kernel and an anillic aldehyde crosslinked chitosan housing. A preparation method of the polylactic acid-hydroxyacetic acid copolymer nano-drug carrier is as follows: dispersing a PLGA organic phase which takes dichloromethane and alcohol as a mixed solvent in a water phase to prepare PLGA microspheres by taking PVA (polyvinyl acetate) as an emulsifier by virtue of an one-off emulsion process; then, adding the PLGA microspheres into chitosan liquor, so that the chitosan is adsorbed on the surfaces of the PLGA microspheres, and then adding the chitosan on the surfaces of anillic aldehyde crosslinked PLGA microspheres. The product has a certain pH environmental responsiveness, can realize controlled release of the drug according to in-vivo pH environmental changes, is high in stability, strong in up-taking capacity for microsphere-coated medicaments by the cells, and has very good application prospect in the drug carrier for treating tumors.

Description

technical field [0001] The invention relates to the field of nano-medicine carriers, in particular to a shell-crosslinked polylactic-co-glycolic acid (PLGA) nano-medicine carrier with pH environmental responsiveness and a preparation method and application thereof. Background technique [0002] Tumor is caused by abnormal proliferation of cells, and may spread from the primary site to vital organs and tissues, causing physiological failure of this site and other organs, and finally leading to death of the human body. Therefore, cancer is one of the major diseases currently endangering human life and health. Chemotherapy is one of the most commonly used and effective methods for treating tumors. Traditional chemotherapy is to inject drugs directly into the body through oral or intravenous injection. The drugs reach the tumor site and enter the tumor cells during the blood circulation to achieve the purpose of treatment. However, in the process of circulation in the body, on...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/36B82Y5/00C08J3/24A61P35/00
Inventor 刘杰蒋庆杨哲路振平甘盛龙
Owner SUN YAT SEN UNIV
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