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PLGA-PEG-ZOL drug-loaded nano-material specifically targeting bone tissuse, and preparation method thereof

A PLGA-PEG-ZOL, drug-loaded nanotechnology, applied in the direction of pharmaceutical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of widespread use and delay the onset Burst-release dose, ease of handling, effects of increasing drug stability and solubility

Active Publication Date: 2019-02-01
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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  • PLGA-PEG-ZOL drug-loaded nano-material specifically targeting bone tissuse, and preparation method thereof
  • PLGA-PEG-ZOL drug-loaded nano-material specifically targeting bone tissuse, and preparation method thereof
  • PLGA-PEG-ZOL drug-loaded nano-material specifically targeting bone tissuse, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 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.

[0043] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0044] (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

[0061] 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.

[0062] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0063] (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

[0067] 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.

[0068] The preparation method of the PLGA-PEG-ZOL drug-loaded nanomaterial specifically targeting bone tissue in this embodiment comprises the following steps:

[0069](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 nano-material specifically targeting bone tissues. The shell surface of PLGA is coupled with zoledronic acid, so the obtained PLGA has the in vivo targeting ability to actively target the bone tissues, and the PLGA has a treatment effect on osteoporosis and osteolysis, so the obtained PLGA can be used as a drug carrier shell to encapsulate a therapeutic drug in order to delay the initial burst release dose of the drug, prolong the half-life of the drug and increase the stability and the solubility of the drug, and enables nanoparticles to havea certain sustained release effect and a passive targeting property, that is, the PLGA-PEG-ZOL drug-loaded nano-material can be loaded with different drugs and target the drugs to the bone tissues according to different treatment demands in order to increase the drug concentration of the drugs in bone tissues, thereby the nano-material has the potential to be suitable for multiple skeletal systemdiseases. The invention also discloses a preparation method of the drug-loaded nanomaterial. The preparation method has the advantages of simple process, and easiness in operation.

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 Applications(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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