Nano-drug with photothermal fast and controlled release and preparation method thereof

A nano-drug and fast technology, applied in the field of controlled-release nano-drug and its preparation, can solve the problems of slow rate and poor therapeutic effect, and achieve the effect of improving the therapeutic effect and improving the efficiency of drug utilization

Active Publication Date: 2022-01-04
HUAIYIN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some nanoparticle drugs currently disclosed have a slow release rate in the process of releasing their loaded drugs, which may easily lead to poor therapeutic effects. important requirement

Method used

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  • Nano-drug with photothermal fast and controlled release and preparation method thereof
  • Nano-drug with photothermal fast and controlled release and preparation method thereof
  • Nano-drug with photothermal fast and controlled release and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] 1) furanization (PCL-Fur) of polycaprolactone: get 0.5 mmol of polycaprolactone (molecular weight is 5K Da) and dissolve in acetone, then add potassium carbonate, n-tetrabutylammonium bromide and Dibromomethylfuran was heated under reflux at 65°C for 48 hours to obtain polycaprolactone PCL-Fur with a furyl group at one end;

[0028] 2) Preparation of carrier (PCL-DA-PEG): Take 0.1 mmol of PCL-Fur and 0.1 mmol of maleimide-based polyethylene glycol (molecular weight 5K Da), add to N,N-dimethyl In a formamide solvent, heat and stir at 40° C. for 48 hours to obtain a PCL-DA-PEG carrier.

[0029] 3) Preparation of photothermal rapid controlled-release nanomedicine: Take PCL-DA-PEG, doxorubicin and copper sulfide nanoparticles in a mass ratio of 10:5:3 and dissolve them in dichloromethane, and drop them into into 10 times the volume of deionized water, after ultrasonic emulsification, the dichloromethane in the system was removed by rotary evaporation, and after centrifugal...

Embodiment 2

[0031] 1) furanization (PCL-Fur) of polycaprolactone: get 0.5 mmol of polycaprolactone (molecular weight is 2K Da) and dissolve in acetone, add potassium carbonate, n-tetrabutylammonium bromide and Dibromomethylfuran was heated under reflux at 60°C for 40 hours.

[0032] 2) Preparation of carrier (PCL-DA-PEG): Take 0.1mmol of PCL-Fur and 0.12mmol of maleimide-based polyethylene glycol (molecular weight 2K Da), add to N,N-dimethyl In a formamide solvent, heat and stir at 30° C. for 40 hours to obtain a PCL-DA-PEG carrier.

[0033] 3) Preparation of photothermal rapid controlled-release nanomedicine: Take PCL-DA-PEG, doxorubicin, and gold nanorods in a mass ratio of 10:2:2 and dissolve them in dichloromethane, and drop them into the 10 times the volume of deionized water, after ultrasonic emulsification, the dichloromethane in the system was removed by rotary evaporation, and after centrifugal cleaning, freeze-dried to obtain nano drug powder with a particle size of about 70nm....

Embodiment 3

[0035] 1) furanization (PCL-Fur) of polycaprolactone: get 0.5 mmol of polycaprolactone (molecular weight is 5K Da) and dissolve in acetone, add potassium carbonate, n-tetrabutylammonium bromide and Dibromomethylfuran was heated under reflux at 70°C for 50 hours.

[0036] 2) Preparation of the carrier (PCL-DA-PEG): Take 0.1 mmol of PCL-Fur and 0.11 mmol of maleimide-based polyethylene glycol (molecular weight 2K Da), add to N,N-dimethyl In a formamide solvent, heat and stir at 50° C. for 50 hours to obtain a PCL-DA-PEG carrier.

[0037] 3) Preparation of photothermal rapid controlled-release nanomedicine: Take PCL-DA-PEG, paclitaxel, and gold nanorods in a mass ratio of 10:5:3 and dissolve them in dichloromethane. After fully dissolving, drop them into 8 times volume of deionized water, after ultrasonic emulsification, the dichloromethane in the system was removed by rotary evaporation, and after centrifugal cleaning, freeze-dried to obtain nano drug powder with a particle siz...

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Abstract

The invention discloses a nano-medicine with photothermal rapid and controlled release and a preparation method thereof. The nano-medicine includes a carrier, an active drug loaded on the carrier and a near-infrared photothermal conversion material; the carrier is polycaprolactone with a furyl group at one end and A polymer covalently bonded with maleimide-based polyethylene glycol; the preparation method is to prepare a carrier from furylated polycaprolactone and maleimide-based polyethylene glycol as raw materials, and include Materials and active drugs with light-to-heat conversion capability. The nano-medicine prepared by the present invention can quickly realize the rapid and controlled release of the drug under near-infrared light, improve the utilization efficiency of the drug, and can also realize the combined treatment of chemotherapy and photothermal therapy, thereby greatly improving the therapeutic effect of tumors.

Description

technical field [0001] The invention relates to a controlled-release nano-medicine and its preparation, in particular to the synthesis of an amphiphilic copolymer constituting a drug carrier, as well as a photothermal rapid controlled-release nano-medicine and a preparation method thereof. Background technique [0002] As a carrier of chemotherapeutic drugs, drug carriers must quickly release the loaded drugs after they are delivered to the target, which is a basic requirement for drug carriers, especially drug carriers for tumor therapy. There are many reasons for this. First of all, tumor cells have both intrinsic drug resistance mechanisms and acquired drug resistance mechanisms, which enable them to exclude intracellular drugs from the cells or alleviate the effects of chemotherapy drugs on tumors through a series of detoxification mechanisms. Cell lethality, so this requires a higher drug concentration in tumor cells; on the other hand, the endocytosis of drug carriers ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K41/00A61K31/704A61K31/337A61K31/4745A61P35/00
CPCA61K9/5153A61K9/5192A61K41/0052A61K31/704A61K31/337A61K31/4745A61P35/00A61K2300/00
Inventor 沈灿柳森叶玮潘长江杨忠美魏言春权莉张超刘静静
Owner HUAIYIN INSTITUTE OF TECHNOLOGY
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