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A kind of plga-peg-zol drug-loaded nanomaterial specifically targeting bone tissue and its preparation method

A technology of PLGA-PEG-ZOL and drug-loaded nanometers, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of wide use and release, and achieve easy operation, The effect of delayed burst release dose and simple process

Active Publication Date: 2021-12-28
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the targeted therapy research of drug-loaded nanotechnology belongs to the field of tumors, and has not been widely used in clinical practice.
The research on the technology of drug-loaded nanomaterials for the skeletal system is still in its infancy, and further in-depth exploration is needed

Method used

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  • A kind of plga-peg-zol drug-loaded nanomaterial specifically targeting bone tissue and its preparation method
  • A kind of plga-peg-zol drug-loaded nanomaterial specifically targeting bone tissue and its preparation method
  • A kind of plga-peg-zol drug-loaded nanomaterial specifically targeting bone tissue and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A kind of PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue of the present invention, such as figure 1 As shown, polylactic acid-glycolic acid is used as the matrix of drug-loaded nanomaterials, and zoledronic acid is coupled to the surface of the matrix; the chemical formula of PLGA-PEG-ZOL is Wherein, 5≤n≤100, 5≤x≤100, 5≤y≤100.

[0042] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0043] (1) With polylactic acid-glycolic acid (2g, 0.02mmol) and diaminopolyethylene glycol (0.8g, 0.04mmol) as substrates, dicyclohexylcarbodiimide (0.049g, 0.24mmol) and N -Hydroxysuccinimide (0.027g, 0.024mmol) is used as a dehydrating agent, and 100ml of toluene is used as a solvent. All the above-mentioned substances are added in a 250ml single-necked flask, and a water separator and a reflux condenser flask are connected to the flask. Heating to 140°C ...

Embodiment 2

[0060] A kind of PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue of the present invention, such as figure 1 As shown, polylactic acid-glycolic acid is used as the matrix of drug-loaded nanomaterials, and zoledronic acid is coupled to the surface of the matrix; the chemical formula of PLGA-PEG-ZOL is Wherein, 5≤n≤100, 5≤x≤100, 5≤y≤100.

[0061] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0062] (1) With polylactic acid-glycolic acid (2g, 0.02mmol) and diaminopolyethylene glycol (1g, 0.05mmol) as substrates, dicyclohexylcarbodiimide (0.074g, 0.36mmol) and N- Hydroxysuccinimide (0.020g, 0.018mmol) is used as a dehydrating agent, and 150ml of toluene is used as a solvent. All the above-mentioned substances are added in a 250ml single-necked flask, and the water separator and the reflux condenser flask are connected to the flask, and heated The ...

Embodiment 3

[0066] A kind of PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue of the present invention, such as figure 1 As shown, polylactic acid-glycolic acid is used as the matrix of drug-loaded nanomaterials, and zoledronic acid is coupled to the surface of the matrix; the chemical formula of PLGA-PEG-ZOL is Wherein, 5≤n≤100, 5≤x≤100, 5≤y≤100.

[0067] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0068](1) With polylactic acid-glycolic acid (2g, 0.02mmol) and diaminopolyethylene glycol (0.8g, 0.04mmol) as substrates, dicyclohexylcarbodiimide (0.061g, 0.3mmol) and N -Hydroxysuccinimide (0.022g, 0.02mmol) is used as a dehydrating agent, and 100ml of toluene is used as a solvent. All the above-mentioned substances are added in a 250ml single-necked flask, and a water separator and a reflux condenser flask are connected to the flask. Heating to 140°C for...

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Abstract

The invention discloses a PLGA‑PEG‑ZOL drug-loaded nanomaterial specifically targeting bone tissue, which is coupled with zoledronic acid on the surface of the PLGA shell, which not only has the ability to actively target bone tissue in vivo, but also has The effect of treating osteoporosis and osteolysis can be used as a drug carrier shell, which encapsulates therapeutic drugs, can delay the initial burst release dose of drugs, prolong the half-life of drugs, increase drug stability and solubility, and enable nanoparticles to have Certain slow-release effect and passive targeting, that is, according to different treatment needs, PLGA-PEG-ZOL drug-loaded nanomaterials are loaded with different drugs, targeting these drugs to bone tissue, and increasing the drug concentration of these drugs in bone tissue , so it has the potential to be applied to a variety of skeletal system diseases. It also discloses a preparation method of the drug-loaded nanometer material, which has a simple process and is easy to operate.

Description

technical field [0001] The invention belongs to the technical field of targeting materials, and in particular relates to a PLGA-PEG-ZOL drug-loaded nanometer material specifically targeting bone tissue and a preparation method thereof. Background technique [0002] Because the blood circulation of bone tissue in many parts of the human body is not rich (such as subchondral bone, skull, etc.), the way of intravenous administration often makes the bone tissue of the diseased part fail to reach an effective blood drug concentration; Drugs reach the lesion in a concentrated manner, but repeated local injections will not only aggravate the pain of the patient, but also greatly increase the risk of infection, leading to serious complications. Therefore, how to increase the blood concentration of therapeutic drugs in the bone tissue of the lesion and improve the therapeutic effect is an important scientific problem urgently needed to be solved in orthopedics. [0003] Drug-loaded ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/59A61K47/60A61K31/675A61K47/34A61P19/10C08G63/91
CPCA61K47/34A61K47/593A61K47/60A61P19/10A61K31/675C08G63/912
Inventor 汪龙牛诚诚安森博胡懿郃
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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