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Nanoparticle and preparation method thereof

A nanoparticle and phospholipid technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, bulk delivery, etc., can solve the problems of short half-life of polymer nanoparticles, easy aggregation of particles, and inability to be effectively solved.

Inactive Publication Date: 2010-05-19
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the half-life of polymer nanoparticles is short, and the introduction of hydrophilic polymer polyethylene glycol (PEG) for modification cannot be effectively solved. At the same time, the particles are easy to agglomerate, which increasingly constitutes a technical bottleneck in the development and application of polymer nanoparticles.
Nanoliposomes also have obvious defects, such as the low encapsulation efficiency of strongly hydrophobic components, and the need for multi-step preparation and purification are also problems that have not been solved.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1), get appropriate amount of PLGA and be dissolved in acetocyanide, obtain PLGA acetocyanide solution, concentration is 2mg / ml;

[0023] (2) Take 0.06mg of DSPE-PEG-COOH and 0.24mg of soybean lecithin, add them to 3ml of 4% ethanol aqueous solution, heat and stir to 65°C to obtain a mixed ethanol aqueous solution;

[0024] (3) Add 1ml of PLGA acetocyanide solution dropwise to 3ml of the above-mentioned mixed ethanol aqueous solution, and continuously stir at 65°C for 2 hours, during which time the solvent is allowed to volatilize, and PLGA-phospholipid-PEG nanometers with an average diameter of 80-250nm are obtained. particles.

Embodiment 2

[0026] Add 1ml of PLGA acetocyanide solution dropwise to 1.5ml of mixed ethanol aqueous solution, the others are the same as in Example 1, and finally obtain PLGA-phospholipid-PEG nanoparticles with an average diameter of 80-250nm.

Embodiment 3

[0028] Add 1ml of PLGA acetocyanide solution dropwise to 6ml of mixed ethanol aqueous solution, the others are the same as in Example 1, and finally obtain PLGA-phospholipid-PEG nanoparticles with an average diameter of 80-250nm.

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Abstract

The invention relates to a nanoparticle and a preparation method thereof. Poly(lactide-glycolide acid) (PLGA) is in the center to serve as a core, phospholipid surrounds the surface of the PLGA core in monolayer and distearoyl phosphatidylethanolamine-polyethyleneglycol-carboxyl (DSPE-PEG-COOH) penetrates the monolayer phospholipid to serve as the shell. The phospholipid, the DSPE-PEG-COOH and the PLGA have good biocompatibility, can entrap hydrophobic drugs and control the drugs to release slowly in the human bodies. The phospholipid surrounds the surface of the PLGA, thus ensuring that the particle can avoid immune system recognition so that the circulating half life of the particle is lengthened. The PEG shell ensures the particle to have spatial stability, static stability, long circulation and other characteristics and to be not easily agglomerated. Meanwhile, carboxyl is easily crosslinked with such ligands as antibodies, peptide, probes and the like, thus ensuring the particle to have targeting characteristic. The preparation method of the nanoparticle is simple, convenient practical and is easy to operate and popularize.

Description

【Technical field】 [0001] The invention relates to the field of drug carriers, in particular to a nanoparticle and a preparation method thereof. 【Background technique】 [0002] Two types of mainstream nanocarriers represented by polymer nanoparticles and nanoliposomes can efficiently encapsulate and transport drugs, genes, etc., and have become a research hotspot for scientists from all over the world. Polyglycolide lactide (PLGA), polylactic acid, polycaprolactone and other polymer nanoparticles have the advantages of good biocompatibility, controllable biodegradation, low toxicity of degradation products, and easy target-controlled release. It is increasingly favored, and some products have been put into the market and clinical trials. Nano-liposomes have a biomembrane structure of phospholipid bilayers, have excellent hydrophilicity, lipophilicity and natural targeting, long-term, and inclusive properties, and are non-toxic, non-immunogenic, and absorbable. Fast speed, h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34
Inventor 蔡林涛龚萍郑明彬贾冬雪
Owner SHENZHEN INST OF ADVANCED TECH
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