Novel bone-target nano-particle with high affinity and method for preparing novel bone-target nano-particle

A kind of affinity and nanoparticle technology, applied in the field of medical materials, can solve the problems of not being able to participate in human metabolism, infectious diseases and tumors, and non-degradable materials, so as to prolong the drug action time, good tissue compatibility, and effective bone tissue delivery effect

Inactive Publication Date: 2019-01-04
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Autologous bone transplantation is limited by the limitation of its own donors, and the second operation brings pain to the patient; allogeneic bone transplantation mainly has immune rejection, which may lead to infectious diseases and tumor formation; Artificial bone subs

Method used

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  • Novel bone-target nano-particle with high affinity and method for preparing novel bone-target nano-particle
  • Novel bone-target nano-particle with high affinity and method for preparing novel bone-target nano-particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of PLGA-b-PEG-TC nanoparticles loaded with simvastatin, wherein simvastatin 2mg, PLGA-b-PEG-TC 20mg

[0031] Specifically, the following steps are included:

[0032] (1) Synthesis of PLGA-b-PEG-COOH polymer

[0033] Dissolve PLGA-COOH, NHS and EDC in dichloromethane according to the addition amount of 1 mg, 1 mg, and 1.5 mg to react to generate PLGA with active ends, and then drop the generated PLGA with active ends into ether to precipitate, and use The precipitate was repeatedly washed with ice ether and methanol mixture to remove the remaining catalyst, and the precipitate was dried in a vacuum oven; after that, 1 g of PLGA with active ends was accurately weighed and dissolved in tetrachloromethane, and then 250 mg of NH2-PEG was added -COOH and 28mg N,N-diisopropylethylamine, after magnetic stirring for 12 hours, the product was gradually dropped into methanol to precipitate, and the precipitate was washed repeatedly with ice methanol 3 times to remove ...

Embodiment 2

[0041] Preparation of PLGA-b-PEG-TC nanoparticles loaded with simvastatin, wherein simvastatin 2.5mg, PLGA-b-PEG-TC 20mg

[0042] Specifically, the following steps are included:

[0043] (1) Synthesis of PLGA-b-PEG-COOH polymer

[0044] Dissolve PLGA-COOH, NHS and EDC in dichloromethane according to the addition amount of 1 mg, 1 mg, and 1.5 mg to react to generate PLGA with active ends, and then drop the generated PLGA with active ends into ether to precipitate, and use The iced ether and methanol mixture repeatedly washed the precipitate to remove the remaining catalyst. After that, the precipitate was dried in a vacuum oven; finally, 1 g of PLGA with active ends was accurately weighed and dissolved in tetrachloromethane, and then 250 mg of NH2- PEG-COOH and 28mg N,N-diisopropylethylamine were reacted with magnetic stirring for 12 hours, and the product was gradually dropped into methanol to precipitate, and the precipitate was washed repeatedly with ice methanol for 3 time...

Embodiment 3

[0050] Preparation of simvastatin-loaded PLGA-b-PEG-TC nanoparticles, wherein simvastatin 3mg, PLGA-b-PEG-TC 20mg

[0051] Specifically, the following steps are included:

[0052] (1) Synthesis of PLGA-b-PEG-COOH polymer

[0053] Dissolve PLGA-COOH, NHS and EDC in dichloromethane according to the addition amount of 1 mg, 1 mg, and 1.5 mg to react to generate PLGA with active ends, and then drop the generated PLGA with active ends into ether to precipitate, and use The iced ether and methanol mixture repeatedly washed the precipitate to remove the remaining catalyst. After that, the precipitate was dried in a vacuum oven; finally, 1 g of PLGA with active ends was accurately weighed and dissolved in tetrachloromethane, and then 250 mg of NH2- PEG-COOH and 28mg N,N-diisopropylethylamine were reacted with magnetic stirring for 12 hours, and the product was gradually dropped into methanol to precipitate, and the precipitate was washed repeatedly with ice methanol for 3 times to re...

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Abstract

The invention provides a novel bone-target nano-particle with high affinity and a method for preparing the novel bone-target nano-particle. The novel bone-target nano-particle comprises PLGA-PEG-COOHpolymer medicine carriers, a bone-target substance tetracycline and hydrophobic medicines. The novel bone-target nano-particle and the method for preparing the novel bone-target nano-particle with thehigh affinity have the advantages that PLGA-b-PEG-COOH polymers can be generated by polymers PLGA-COOH and NH2-PEG-COOH under the effects of EDC/NHS catalysts, surface modification is carried out bythe tetracycline, carriers have bone tissue target performance by the aid of the bone deposition ability of the tetracycline, and accordingly anti-osteoporosis medicines can be effectively delivered to bone tissues; the carriers have the bone tissue target performance by the aid of the bone deposition ability of the tetracycline, and accordingly the anti-osteoporosis medicines can be effectively delivered to the bone tissues.

Description

technical field [0001] The invention belongs to the technical field of medical materials, and in particular relates to a novel bone-targeting nanoparticle with high affinity and a preparation method thereof. Background technique [0002] Osteoporosis is a disease of the skeletal system characterized by degeneration of bone tissue microarchitecture, decreased bone mass, increased bone fragility, and increased risk of secondary fractures. The most common symptom of osteoporosis is pain, mainly low back pain. Severe bone pain can affect people's daily life, diet and sleep, etc., often making the patient's life irregular; the severe symptom of osteoporosis is fracture, which is related to Different from ordinary traumatic fractures, osteoporotic fractures are low-energy brittle fractures. While the probability of comminuted fractures is greatly increased, short-term treatment is difficult to be effective, which seriously affects the quality of life of patients. [0003] Bone ti...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K45/00A61K47/28A61P19/10C08G81/00A61K31/546A61K31/366A61K31/704A61K31/192A61K31/7048
CPCA61K9/5153A61K31/192A61K31/366A61K31/546A61K31/704A61K31/7048A61K45/00A61K47/28A61P19/10C08G81/00
Inventor 魏坤严柳柳胡方斌牛雪明莫灿龙杨业国
Owner SOUTH CHINA UNIV OF TECH
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