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Polylactic acid-hydroxyacetic acid copolymer nano-drug carrier as well as preparation method and application thereof

A glycolic acid copolymer, nano-drug carrier technology, applied in nano-drugs, nano-technology, nano-technology and other directions, can solve the problems of poor drug absorption effect, weak cell uptake ability, lack of specific binding, etc., to achieve enhanced Drug treatment effect, enhancement of cellular uptake capacity, effect of enhanced uptake capacity

Active Publication Date: 2014-08-27
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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  • Polylactic acid-hydroxyacetic acid copolymer nano-drug carrier as well as preparation method and application thereof
  • Polylactic acid-hydroxyacetic acid copolymer nano-drug carrier as well as preparation method and application thereof
  • Polylactic acid-hydroxyacetic acid copolymer nano-drug carrier as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0050] PLGA was dissolved in a mixture of dichloromethane and ethanol at a volume ratio of 3:1 to prepare a PLGA solution with a concentration of 20 mg / mL. The above PLGA solution was dropped into a 0.75% mass percent PVA aqueous solution under the condition of vortex oscillation, and phacoemulsified 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 hours to solidify the nanospheres. The nanospheres were centrifuged at 4°C and 13000 rpm for 10 min and washed twice to obtain product P. Using aqueous acetic acid as the solvent, chitosan solutions with concentration gradients of 1.25 mg / mL, 2.5 mg / mL, and 3.75 mg / mL were prepared and adjusted to pH=6.0. Disperse the collected microspheres in the above chitosan solutions of different concentrations, stir for 3 hours to make the chitosan ...

Embodiment 2

[0053] Dissolve PLGA 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; prepare an aqueous solution of chitosan with a concentration of 3.75 mg / mL and adjust the pH to 6.0. The above PLGA solution was dropped into a 0.75% mass percent PVA aqueous solution under the condition of vortex oscillation, and phacoemulsified 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 hours to solidify the nano-microspheres. The nanospheres were centrifuged at 4 ℃ and 13000 rpm for 10 min and washed twice to obtain product P. The collected microspheres were dispersed in the above chitosan aqueous solution, stirred continuously for 3 h, so that the chitosan was adsorbed on the PLGA microspheres, and centrifuged at 4°C...

Embodiment 3

[0056] PLGA was dissolved in a mixture of dichloromethane and ethanol at a volume ratio of 3:1 to prepare a PLGA solution with a concentration of 20 mg / mL. Prepare a chitosan aqueous solution with a concentration of 3.75 mg / mL and adjust the pH to 6.0. The above PLGA solution was dropped into a 0.75% mass percent PVA aqueous solution under the condition of vortex oscillation, and phacoemulsified 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 hours to solidify the nano-microspheres. The nanospheres were centrifuged at 4 ℃ and 13000 rpm for 10 min and washed twice to obtain product P. Disperse the collected microspheres in the above chitosan aqueous solution and stir continuously for 3 hours to make the chitosan adsorb to the PLGA microspheres. Centrifuge at 4 ℃ and 13000 rpm for 10...

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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 cross-linked polylactic acid-glycolic acid copolymer (PLGA) nano-medicine carrier with pH environment responsiveness and a preparation method and application thereof. Background technique [0002] Tumors are caused by abnormal cell proliferation, and may metastasize and spread from the primary site to vital organs and tissues, causing the physiological function of this site and other organs to fail, and finally leading to human death. Therefore, cancer is currently one of the main diseases endangering human life and health. Chemotherapy is currently one of the most commonly used and effective methods to treat 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 blood circulation to achieve the purpose of treatment. However, in the process of circu...

Claims

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Application Information

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Patent Type & Authority Applications(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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