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Hydrogel nanoparticles used as injectable subcutaneous implant agent

A hydrogel and nanoparticle technology, applied in the field of medicine, can solve the problems of difficult to guarantee efficacy or toxicity, high toxicity of anticancer drugs, complicated preparation process, etc., to avoid drug resistance, reduce toxic and side effects, and ensure efficacy. Effect

Inactive Publication Date: 2012-05-23
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The former implant has poor patient compliance, while the latter has high patient compliance, but its preparation process is more complicated, and toxic organic solvents may be used in the preparation process, resulting in organic solvent residues, and it only releases the original drug to the target. parts play a role
However, since breast cancer and other subcutaneous tumors usually require long-term medication, it is easy to develop drug resistance; some anticancer drugs are more toxic, and when they produce high local concentrations, they will also cause high blood drug concentrations, so that the drugs are distributed throughout the body and cause Toxicity; some anticancer drugs target cells inside the cells. For these anticancer drugs, the above two implants are prepared, and the efficacy or toxicity is difficult to guarantee

Method used

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  • Hydrogel nanoparticles used as injectable subcutaneous implant agent
  • Hydrogel nanoparticles used as injectable subcutaneous implant agent

Examples

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Embodiment 1

[0013] The present invention can be provided by following embodiment in concrete implementation:

[0014] 23% polyethylene glycol-poly(lactic-co-glycolic acid) copolymer (wherein the molar ratio of lactic acid / glycolic acid of the poly(lactic-co-glycolic acid) material is 3:1) and 77% water are mixed, placed in the refrigerator to fully swell, into a solution-like hydrogel solution;

[0015] Preparation of stable 2-methoxyestradiol (2ME) liposomes, ether injection method: Weigh 240 mg of soybean lecithin, 24 mg of cholesterol, 10 mg of 2ME into a vial, add 4 ml of ether to dissolve into an oil phase; weigh Poloxamer 1885mg, add 5mlPH 7.4PBS buffer solution to dissolve into the water phase; at 40℃, under 1000r / min magnetic stirring, slowly and uniformly drop the oil phase (inhaled into a 1ml syringe) into the water phase, continue for half an hour to volatilize the diethyl ether and then Continue to stir for 30 minutes to obtain a milky white suspension. After ultrasonicating ...

Embodiment 2

[0017] 23% polyethylene glycol-poly(lactic-co-glycolic acid) copolymer (wherein the molar ratio of lactic acid / glycolic acid of the poly(lactic-co-glycolic acid) material is 3:1) and 77% water are mixed, placed in the refrigerator to fully swell, into a solution-like hydrogel solution;

[0018] To prepare 2-methoxyestradiol solid lipid nanoparticles, weigh 0.48g of glyceryl monostearate and 0.016g of 2-methoxyestradiol and mix them and place them in a water bath at 80°C to melt them completely. Afterwards, stir at 1000rpm speed for 10min as the oil phase; take 0.18g Tween 80, 0.06g poloxamer 188 and 8ml of ultrapure water and mix them and place them in the same water bath to form a solution, which is the water phase; ℃, under the condition of 1000rpm, first add the water phase dropwise to the oil phase at the same temperature at a speed of 10ml / min, and then continue to stir for 10min; Ultrasonic the probe for 8min to obtain the solid lipid nanoparticle suspension of 2-methox...

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Abstract

The invention relates to hydrogel nanoparticles used as an injectable subcutaneous implant agent, which can effectively solves the problem of fulfilling an aim of realizing tumor treatment by locally injecting the hydrogel nanoparticles beside a subcutaneous tumor, changing the hydrogel nanoparticles into a gel and slowly releasing nanoparticles in vivo. The hydrogel nanoparticles are prepared from hydrogel solution and 2-methoxyl estradiol liposome nanoparticle powder or solid liposome nanoparticle powder by a method which comprises the following steps of: adding the 2-methoxyl estradiol liposome nanoparticle powder or the solid liposome nanoparticle powder into the hydrogel solution; and uniformly mixing to form the hydrogel nanoparticles which can be used as an injectable subcutaneous implant agent, wherein 100mg of the 2-methoxyl estradiol liposome nanoparticle powder is added into every 1ml of the hydrogel solution. The injectable hydrogel implant agent of the invention can be used for treating subcutaneous tumors such as breast cancer and the like, keep an effective medicament concentration in a local target site, can realize sustained release and controlled release, can avoid medicament resistance caused by long-term medication, simultaneously improve a curative effect and reduce dosage, reduce toxic and side effects on a whole body, and also can prevent lymphatic metastasis of the tumors such as the breast cancer and the like.

Description

1. Technical field [0001] The invention relates to medicine, in particular to a nanoparticle hydrogel used as an injectable subcutaneous implant. 2. Background technology [0002] Implants for subcutaneous tumor therapy are currently generally in the form of solids that require minor surgery to implant subcutaneously for efficacy or locally injectable suspensions of microspheres. The former implant has poor patient compliance, while the latter has high patient compliance, but its preparation process is more complicated, and toxic organic solvents may be used in the preparation process, resulting in organic solvent residues, and it only releases the original drug to the target. parts function. However, since breast cancer and other subcutaneous tumors usually require long-term medication, it is easy to develop drug resistance; some anticancer drugs are more toxic, and when they produce high local concentrations, they will also cause high blood drug concentrations, so that th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/565A61K47/34A61P35/00
Inventor 张振中郭新红李俊梅张鑫鑫张正全胡海英邢亚兵梅芊
Owner ZHENGZHOU UNIV
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