Preparation method of targeting composite nanoparticle

A nanoparticle and composite technology, which is applied in the research field of hydroxycamptothecin-loaded targeted nanoparticles, can solve the problems of drugs that can only be dissolved in acetonitrile, drug stability, encapsulation efficiency, product drug loading The problem of low dosage and encapsulation efficiency can be achieved to prolong the effective time of action, promote the combination, and achieve the effect of large drug loading

Active Publication Date: 2012-11-14
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

First of all, the solvent needs to be heated to 65 degrees Celsius during the preparation process, which is higher than the glass transition temperature of PLGA, which will affect the molecular chain of the carrier material. If it is used for the preparation of drug-loaded nanoparticles, it may affect the stability of the drug. properties and encapsulation efficiency; secondly, if drug-loaded nanoparticles are to be prepared by this method, it can only target drugs that can be dissolved in ace

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  • Preparation method of targeting composite nanoparticle
  • Preparation method of targeting composite nanoparticle
  • Preparation method of targeting composite nanoparticle

Examples

Experimental program
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Effect test

Embodiment 1

[0033]Dissolve PLGA in an organic solvent with a volume ratio of dichloromethane: ethanol = 3:1 to form an organic solution with a concentration of 50 mg / mL. The mass ratio of lecithin and polyethylene glycol-distearoylphosphatidylethanolamine is 9: 1 Dissolve in the above organic solution, and add it dropwise to 2 times the volume of ultrapure water, use an ultrasonic cell breaker with a power of 7W, ultrasonic for 30 seconds, then add the emulsion to 2 times the volume of ultrapure water, continuously Stir for 3 hours to remove the organic solvent, solidify and shape the composite nanoparticles, and finally collect by centrifugation, wash with ultrapure water three times, and freeze-dry to obtain composite nanoparticles.

[0034] Laser particle size analysis showed that the obtained nanoparticles were normally distributed with an effective diameter of 357 nm and a polydispersity of 0.268. Observed under a scanning electron microscope, the nanoparticles have a regular spheric...

Embodiment 2

[0036] Dissolve PLGA in an organic solvent with a volume ratio of dichloromethane: ethanol = 4:1 to form an organic solution with a concentration of 40 mg / mL, lecithin and polyethylene glycol-distearoylphosphatidylethanolamine in a mass ratio of 7: 3 Dissolve in the above organic solution, add it dropwise to 2 times the volume of ultrapure water, use an ultrasonic cell breaker with a power of 9W, ultrasonicate for 60 seconds, then add the emulsion to 2 times the volume of ultrapure water, and continue stirring for 3 hours The organic solvent is removed, the composite nanoparticles are solidified and formed, finally collected by centrifugation, washed three times with ultrapure water, and freeze-dried to obtain composite nanoparticles.

[0037] Laser particle size analysis showed that the obtained nanoparticles were normally distributed with an effective diameter of 337 nm and a polydispersity of 0.228. Observed under a scanning electron microscope, the nano-microspheres have a...

Embodiment 3

[0039] Dissolve PLGA in an organic solvent with a volume ratio of dichloromethane: ethanol = 5:1 to form an organic solution with a concentration of 30 mg / mL, lecithin and polyethylene glycol-distearoylphosphatidylethanolamine in a mass ratio of 5: 5 Dissolve in the above organic solution, add it dropwise to 4 times the volume of ultrapure water, use an ultrasonic cell disruptor with a power of 11W, and ultrasonicate for 120 seconds, then add the emulsion to 4 times the volume of ultrapure water, and continue stirring for 3 hours The organic solvent is removed, the composite nanoparticles are solidified and formed, finally collected by centrifugation, washed three times with ultrapure water, and freeze-dried to obtain composite nanoparticles.

[0040] Laser particle size analysis showed that the obtained nanoparticles were normally distributed with an effective diameter of 305 nm and a polydispersity of 0.186. Observed under a scanning electron microscope, the nano-microsphere...

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Abstract

The invention discloses a preparation method of targeting composite nanoparticle. The invention uses phospholipids, pegylated phospholipids and polyethylene glycol-distearoyl phosphatidyl ethanolamine connected with RGD (arginine-glycine-aspartic acid) as an emulsifier, and uses a binary mixture solvent system of dichloromethane and ethanol to prepare the targeting composite nanoparticle which contains PLGA (poly lactic-co-glycolic acid) as the nucleus and contains the phospholipids and pegylated phospholipids as a shell by one-step emulsification method. The invention uses the hydroxyl camptothecin as a model drug to prepare the RGD targeting phospholipid-polymer composite nanoparticle with high drug loading rate (18.9%) and high entrapment efficiency (94.5%). The phospholipid monolayer and polyethylene glycol hydration layer located on the surface of the targeting composite nanoparticle prepared by the method provided by the invention can significantly reduce protein adsorption and extend the action time in vivo; the RGD connected with the shell of the composite nanoparticle can effectively promote nanoparticles specific binding to tumor cells or tumor new vessels with high expression of integrin, and improve the local drug concentration, so as to enable the targeting composite nanoparticles to have a better anti-tumor effect.

Description

technical field [0001] The invention belongs to the field of nano-medicine carriers, and in particular relates to a preparation process of targeted lipid-polymer composite nanoparticles and research on targeted nanoparticles loaded with hydroxycamptothecin. Background technique [0002] Malignant tumors are currently the most serious disease threatening human health and have become the number one cause of human death. At present, the treatment methods for malignant tumors mainly include surgery, chemotherapy, radiation therapy, etc. Among them, chemotherapy is the most suitable treatment method in addition to surgery in clinical practice, and its application is very common. Most chemotherapy drugs not only kill tumor cells, but also destroy normal tissues and cells, resulting in serious side effects. Therefore, the use of nanoparticles as drug carriers is one of the most effective means to reduce the toxic and side effects of chemotherapy drugs and improve the efficacy of d...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K47/24A61K31/4745A61P35/00
Inventor 刘杰蒋庆杨哲
Owner SUN YAT SEN UNIV
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