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Nanoparticle for microwave touch release of PLGA shell, and preparation method and application of nanoparticle

A nanoparticle, PLGA technology, applied in wave energy or particle radiation treatment materials, medical preparations without active ingredients, medical preparations containing active ingredients, etc. and other problems, to achieve the effect of reducing the cost of use and low price

Pending Publication Date: 2020-07-17
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As an important class of nanoparticle shell materials, PLGA has good biological safety and stability, but it also has a low release rate of therapeutic drugs contained in it, and cannot achieve effective enrichment of therapeutic drugs in the target area, which limits its application.
[0003] In the field of drug touch release, it includes endogenous touch release and exogenous touch release. Among them, endogenous touch release includes pH response and enzyme response, but its main disadvantage is that it does not affect the endogenous pH of the target tissue. Value change, response enzyme content, etc. have a strong dependence, and human intervention, control intensity, etc. cannot be performed
Exogenous touch release includes optical response and magnetic response, but the penetration depth of the optical response is low (about 10mm). When the distance between the local tissue lesion and the surface of the body is greater than 1cm, it is impossible to trigger the nanometers gathered in the target area. Particles; and magnetic response has the disadvantages of large and expensive equipment required for touch release
Therefore, for drugs with large systemic side effects, the effective enrichment in the target area cannot be effectively achieved, and it is easy to cause side effects on the human body. Therefore, a low-cost nanoparticle that can effectively achieve effective enrichment in the drug-loaded target area is needed.

Method used

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  • Nanoparticle for microwave touch release of PLGA shell, and preparation method and application of nanoparticle
  • Nanoparticle for microwave touch release of PLGA shell, and preparation method and application of nanoparticle
  • Nanoparticle for microwave touch release of PLGA shell, and preparation method and application of nanoparticle

Examples

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preparation example Construction

[0037] The present invention also provides a method for preparing the nanoparticles of the microwave touch release PLGA shell, comprising the following steps:

[0038] (a) Weighing the materials used to form the shell of nanoparticles and placing them in a centrifuge tube, adding dichloromethane or trichloromethane to form a solution. Preferably, the material used to form the nanoparticle shell in the step (a) includes PLGA or PLGA and DPPC. Preferably, the mass ratio of PLGA to DPPC is 2:1.

[0039] (b) The microwave sensitizer is mixed with pure water or ultrapure water to form a solution. Preferably, the volume ratio of microwave sensitizer to pure water or ultrapure water is 1:1 or 1:2.

[0040] (c) adding the microwave sensitizer solution formed in step (b) to the centrifuge tube of step (a);

[0041](d) Place the centrifuge tube in an ice bath, and use ultrasonic cell disruption to disperse the mixed liquid in the centrifuge tube. Preferably, the dispersion time is 2...

Embodiment 1

[0052] In Example 1, microwave touch release nanoparticles with PLGA as the outer shell and microwave sensitizer 1-butyl-3-methylimidazole L-lactate were prepared. The preparation method is as follows:

[0053] 1) Weigh 20mg of PLGA into a 50ml centrifuge tube, add 2ml of dichloromethane to form a solution.

[0054] 2) Mix the microwave sensitizer 1-butyl-3-methylimidazole L lactate with pure water at a volume ratio of 1:1 to form a solution.

[0055] 3) Add 200 μL of the solution in step 2) into the 50 ml centrifuge tube in step 1).

[0056] 4) Put the above 50ml centrifuge tube in an ice bath, use an ultrasonic cell disruptor to disperse the mixed liquid in the 50ml centrifuge tube, the dispersion time is 2min, instrument parameters: power 98w, 50% duty cycle.

[0057] 5) Weigh 0.2 mg of polyvinyl alcohol powder and add 10 ml of pure water to prepare a 4% polyvinyl alcohol solution.

[0058] 6) Add 10 ml of 4% polyvinyl alcohol solution into the 50 ml centrifuge tube treat...

Embodiment 2

[0065] In Example 2, microwave touch release nanoparticles with PLGA as the outer shell and microwave sensitizer 1-butyl-3-methylimidazole L-lactate and solid tumor treatment drug paclitaxel were prepared. The preparation method is as follows:

[0066] 1) Weigh 20mg of PLGA and 2mg of paclitaxel into a 50ml centrifuge tube, add 2ml of dichloromethane to form a solution.

[0067] 2) Mix the microwave sensitizer 1-butyl-3-methylimidazole L lactate with pure water at a volume ratio of 1:1 to form a solution.

[0068] 3) Add 200 μL of the liquid in step 2) to the 50ml centrifuge tube in step 1).

[0069] 4) Put the above 50ml centrifuge tube in an ice bath, use an ultrasonic cell disruptor to disperse the mixed liquid in the 50ml centrifuge tube, the dispersion time is 2min, instrument parameters: power 98w, 50% duty cycle.

[0070] 5) Weigh 0.2 mg of polyvinyl alcohol powder and add 10 ml of pure water to prepare a 4% polyvinyl alcohol solution.

[0071] 6) Add 10 ml of 4% poly...

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Abstract

The invention provides a nanoparticle for microwave touch release of a PLGA shell, and a preparation method and application thereof, and relates to the technical field of nanoparticle drug carriers. The nanoparticle at least takes PLGA as a shell, and at least an ionic liquid microwave sensitizer is wrapped in the nanoparticle. Under action of a microwave field, when the prepared nanoparticle formicrowave touch release of the PLGA shell reaches a target tissue, local irradiation is performed on the tissue by using a microwave therapeutic instrument, and the microwave sensitizer in the nanoparticle generates a large amount of heat energy after being irradiated, so that local release of drugs by the nano material is promoted.

Description

technical field [0001] The invention relates to the technical field of nanoparticle drug carriers, in particular to a nanoparticle that releases a PLGA shell by microwave touch control, a preparation method and an application thereof. Background technique [0002] The nanoparticle drug delivery system refers to the use of nanoparticles with a particle size of 1-1000nm as a drug carrier to realize the delivery and release of drugs controlled at the molecular level. Poly(lactic-co-glycolic acid) (poly(lactic-co-glycolic acid), PLGA) is randomly polymerized from two monomers - lactic acid and glycolic acid. It is a degradable functional polymer organic compound with good Biocompatibility, non-toxic, good encapsulation and film-forming properties. As an important class of nanoparticle shell materials, PLGA has good biological safety and stability, but it also has a low release rate of therapeutic drugs contained in it, and cannot achieve effective enrichment of therapeutic drug...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K9/51A61K47/34A61K47/22A61K31/337A61K31/704A61P35/00
CPCA61K41/0028A61K9/5192A61K9/5146A61K9/5123A61K31/337A61K31/704A61P35/00
Inventor 王红徐金顺张欢彭玉兰
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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