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Biocompatibility nanoparticle and application thereof as drug conveying carrier

A nanoparticle, drug-loaded technology, applied in drug combinations, medical preparations with inactive ingredients, antitumor drugs, etc., can solve the problems of low stability, easy dissociation, and inability to improve drug availability and efficacy. , to achieve the effect of enhanced circulation and stability, good hydrophilicity, good biocompatibility and biodegradability

Inactive Publication Date: 2012-06-13
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] A problem that cannot be ignored is that the structure of amphiphilic polymer self-assembled nanoparticles is strongly dependent on the relative ratio of hydrophilic and hydrophobic components, and the stability is not high
As a drug carrier, such self-assembled nanoparticles are prone to dissociation when they are diluted by body fluids or blood, and its disassembly often results in burst release of the drug, which will directly cause the drug to be released before the nanoparticles reach the target site. Therefore, the availability and efficacy of the drug cannot be improved through the EPR effect

Method used

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  • Biocompatibility nanoparticle and application thereof as drug conveying carrier
  • Biocompatibility nanoparticle and application thereof as drug conveying carrier
  • Biocompatibility nanoparticle and application thereof as drug conveying carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1, the synthesis of related compounds

[0050] 1. Synthesis of COP

[0051] Synthesis of 2-chloro-2-oxo-1,3,2-dioxaphospholane (2-chloro-2-oxo-1,3,2-dioxaphospholane, COP) by reaction of phosphorus trichloride with ethylene glycol ), the specific synthesis method is as follows: in a 1000mL three-necked round-bottomed flask, phosphorus trichloride (3.0mol) was dissolved in anhydrous dichloromethane (500mL), and slowly dropped into ethylene glycol through a constant pressure dropping funnel (3.0mol), after all the drops were finished, the reaction was continued for 0.5 hours, the solvent was evaporated under reduced pressure, and the product was evaporated by continuous vacuum distillation twice (50°C, 200Pa). Dissolve the product in benzene and pass through O 2 Reaction for 48 hours, the solvent benzene was evaporated under reduced pressure, and then the product (COP) was evaporated twice by continuous distillation under reduced pressure (88~89°C, 20Pa), and...

Embodiment 2

[0055] Embodiment 2, synthesis and characterization of mPEG-TEGDP nanoparticles

[0056] Schematic diagram of the synthesis of mPEG-TEGDP nanoparticles image 3 shown. Pre-dosed mPEG, TEGDP and Sn(Oct) in a dry round bottom flask 2 , the molar feed ratio of the three and the parameters of the reaction system are shown in Table 1. After the system was reacted for 12 hours, a dialysis bag with a molecular weight of 15,000 was dialyzed in ultrapure water for 72 hours, and a white powder product (mPEG-TEGDP nanoparticle) was obtained after lyophilization.

[0057] Table 1 Synthesis conditions of mPEG-TEGDP nanoparticles

[0058]

[0059] The composition of the nanoparticles was determined using elemental analysis methods. Table 2 shows the elemental analysis results of mPEG-TEGDP nanoparticles, indicating that nanoparticles with different compositions can be obtained by adjusting the synthesis conditions.

[0060] Table 2 Elemental analysis of mPEG-TEGDP nanoparticles

[...

Embodiment 3

[0065] Preparation and characterization of embodiment 3, mPEG-laPEG-TEGDP nanoparticles

[0066] The schematic diagram of the synthesis of mPEG-laPEG-TEGDP nanoparticles is shown in Image 6 shown.

[0067] 1. mPEG-N 3 Preparation of PEG-TEGDP nanoparticles

[0068] mPEG2000, N 3 PEG3400, TEGDP and Sn(Oct) 2 They were added to dry round bottom flasks (see Table 3 for the molar feed ratio). After reacting in dimethyl sulfoxide for 12 hours, dialyze in ultrapure water for 72 hours with a molecular weight of 15,000, and freeze-dry to obtain the surface azide group-functionalized nanoparticles mPEG-N 3 PEG-TEGDP.

[0069] mPEG-N 3 The element ratios of PEG-TEGDP nanoparticles and the calculation results of each component ratio are listed in Table 3. As can be seen from Table 3, N 3 The proportion of PEG in the total amount of initiator increased from 0.9 / 0.1 to 0.5 / 0.5, and its content in nanoparticles also increased, from 0.9 / 0.039 to 0.5 / 0.235. This result indicates tha...

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Abstract

The invention discloses a biocompatibility nanoparticle and an application thereof as a drug conveying carrier. The nanoparticle provided by the invention is shown in (a) or (b): the compound disclosed in the formula (I) of (a) is a shell layer, the compound disclosed in the formula (II) is core nanoparticle, and n1 is equal to 2-400; the compound disclosed in the formula (I) of (b) and the compound disclosed in the formula (III) are shell layers, the compound disclosed in the formula (II) is core nanoparticle, and n2 is equal to 2-400. The invention also provides the preparation method of the nanoparticle, the application and the decorated nanoparticle obtained by decorating the nanoparticle. The nanoparticle obtained by the invention has favorable biocompatibility and biodegradability, which is convenient for further ligand decoration; the nanoparticle is used for targeted conveying of drugs; and nanoparticle decorated by lactose can carry adriamycin to cause adriamycin to effectively enter abnormal cells of liver cancer tissues, so that the treating effect of the nanoparticle is superior to that of the adriamycin. The nanoparticle can be widely applied to the field of drug conveying nanometer carrier. Formula (I), formula (II) and formula (III) are as follows.

Description

technical field [0001] The invention relates to a biocompatible nanoparticle and its application as a drug delivery carrier. Background technique [0002] The study of nano-drug carriers is one of the important directions in the field of nano-biomedical research. A large number of studies have proved that nano-drug carriers can promote the accumulation of drugs in tumor tissues, and the use of nano-drug carriers to deliver drugs has shown good results in cancer treatment and has broad application prospects. Due to the significant difference between the microenvironment of tumor tissue and normal tissue, such as the expansion and bending of blood vessels in tumor tissue, and the lack of lymphatic flow, the pressure inside the tumor tissue is significantly higher than that of the surrounding normal tissue, and a large number of tumor cells proliferate. The anaerobic and low pH environment of tumor tissue is caused, these differences are not conducive to the delivery of small ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/24A61K47/16A61K47/34C08G79/04C08G65/48A61P35/00A61K47/10
Inventor 王均熊梦华吴卷
Owner UNIV OF SCI & TECH OF CHINA
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