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Nanometer drug-loading system as well as preparation method and application thereof

A nano-drug loading and drug-loading nanotechnology, which is applied in the field of nano-drug loading system and its preparation, can solve the problems of large toxic and side effects, large size, and poor biocompatibility, and achieve simple preparation methods, improved sensitivity, and stability high effect

Active Publication Date: 2015-11-11
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the size of the current dual-drug delivery system and photothermal therapy reagents are often relatively large, and it is difficult to control them within 100nm. Moreover, the commonly used photothermal therapy reagents are often gold nanorods, nanocages, carbon materials, biocompatible Poor sex, high toxicity and side effects

Method used

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  • Nanometer drug-loading system as well as preparation method and application thereof
  • Nanometer drug-loading system as well as preparation method and application thereof
  • Nanometer drug-loading system as well as preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0062] In this example, the nano drug-carrying system is prepared by the following method, which specifically includes the following steps:

[0063] (1) 100mgPEG 2000 Disperse -DSPE in 5mL of methanol, stir to dissolve, add 10 mg of doxorubicin in dichloromethane solution (the mass ratio of PEG-DSPE to doxorubicin is 10:1), remove the organic solvent with a rotary evaporator to form a lipid film . Adding a tris-HCl buffer solution at pH 8.5 to the lipid film to form a drug-loaded nanomicelle solution, wherein the drug-loaded PEG-DSPE nanomicelle solution has a concentration of 2 mg / mL;

[0064] (2) Add 20 mg of dopamine hydrochloride to the drug-loaded PEG-DSPE nanomicelle solution obtained in step (1), and stir the reaction container for 24 hours to obtain a drug-loaded PEG-DSPE nanomicelle solution with a core-shell structure, 60000rmp Centrifuge to remove unreacted dopamine and buffer solution, freeze-dry for later use;

[0065] (3) Disperse the lyophilized drug-loaded P...

Embodiment 2

[0068] (1) 100mgPEG 2000-DSPE is dispersed in 6mL aqueous solution, ultrasonically, stirred, add 5mg of doxorubicin hydrochloride (the mass ratio of PEG-DSPE to doxorubicin hydrochloride is 20:1), stir slowly for 2h, then add tris-HCl buffer solution to adjust the pH value to 8.5, the concentration of the tris-HCl buffer solution is 10mmol / L, forming a drug-loaded nanomicelle solution, and making the concentration of the PEG-DSPE nanomicelles 15mg / mL;

[0069] (2) Add 150 mg of dopamine hydrochloride to the drug-loaded PEG-DSPE nanomicelle solution obtained in step (1), and stir and react for 14 hours under the condition that the opening of the reaction vessel is convected with the outside air to obtain drug-loaded PEG-DSPE with a core-shell structure. DSPE nano-micelle solution;

[0070] (3) Add the DMSO solution that is dissolved with 5mg bortezomib in the drug-loaded PEG-DSPE nano-micelle solution that step (2) obtains (the volume ratio of drug-loaded PEG-DSPE nano-micelle...

Embodiment 3

[0073] (1) 100mgPEG 5000 -DSPE was dispersed in 10 mL of tris-HCl buffer solution (pH 8.0) with a concentration of 10 mmol / L to form a PEG-DSPE nano-micelle solution, and then 20 mg of doxorubicin hydrochloride was added and stirred to obtain a drug-loaded nano-micelle solution (loaded The concentration of drug nanomicelle is 10mg / mL);

[0074] (2) Add 10 mL of tris-HCl buffer solution (10 mmol / L, pH 8.0) that is dissolved with 100 mg of dopamine hydrochloride into the drug-loaded PEG-DSPE nanomicelle solution obtained in step (1), and the opening of the reaction vessel is connected to the outside world. Stir and react for 48 hours under air convection to obtain a drug-loaded PEG-DSPE nanomicelle solution with a core-shell structure, centrifuge at 60,000 rpm to remove unreacted dopamine and buffer solution, and freeze-dry for use;

[0075] (3) Add the lyophilized drug-loaded PEG-DSPE nanomicelles to the DMSO / water mixed solution (the volume ratio of water and DMSO is 8:1) dis...

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Abstract

The invention provides a nanometer drug-loading system as well as a preparation method and an application thereof. The nanometer drug-loading system comprises a drug-loading nano-micelle core, a poly-dopamine shell, and bortezomib connected to the poly-dopamine shell, wherein drug-loading nano-micelles are nano-micelles formed by encapsulating chemical anti-cancer drugs by polyethylene glycol-distearoyl phosphoethanolamine. The preparation method of the nanometer drug-loading system comprises the following steps: forming the drug-loading nano-micelles; forming the poly-dopamine shell outside the drug-loading nano-micelles; and connecting bortezomib to the poly-dopamine shell. The nanometer drug-loading system has the grain diameter smaller than 50nm, is high in stability, has a tumor enrichment effect, and realizes simultaneous delivery of bortezomib and other chemical anti-cancer drugs; poly-dopamine has a photothermal effect, can assist chemotherapeutic medicines in treatment, has the synergy of combined treatment of chemotherapy and thermal therapy, and therefore, the nanometer drug-loading system has a wide medical application prospect.

Description

technical field [0001] The invention belongs to the field of nano-biomedicine, and relates to a nano-drug loading system and its preparation method and application. Background technique [0002] Breast cancer is a malignant tumor that seriously affects the health of women. It is mainly caused by the proliferation of malignant cells in the ductal epithelial cells of the mammary glands. Its etiology is not very clear, and it is currently believed that it may be related to changes in heredity, endocrine, viral infection, genes and cytokines. Surgery, radiotherapy, chemotherapy or endocrine therapy are the main treatment methods for breast cancer. However, these treatment methods are not effective, have large toxic and side effects, and poor patient compliance. Studies have shown that photothermal therapy is a low-invasive method that can improve the sensitivity of chemotherapy, and it is expected to cooperate with chemotherapy to improve the anti-tumor effect. [0003] As the...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61K38/05A61K31/704A61K33/24A61K41/00A61K47/34A61K47/48A61K45/00A61P35/00A61K31/337A61K31/675
Inventor 吴雁张瑞锐苏世帅邵磊厚
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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