Unlock instant, AI-driven research and patent intelligence for your innovation.

Amphiphilic base conjugate nanoparticles for treating tumors and preparation method thereof

A nanoparticle and amphiphilic technology, applied in the field of biomedicine, can solve the problems of changing drug properties, affecting drug efficacy, increasing drug cost, etc., and achieving the effects of reducing toxic side effects, avoiding toxic side effects, and avoiding changes in the chemical structure of drugs

Active Publication Date: 2018-08-31
SHANGHAI JIAOTONG UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, many current drug delivery systems involve chemical modification of drugs, which not only increases the cost of drug production, but also easily leads to changes in the properties of the drug itself, thereby affecting the efficacy of the drug.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Amphiphilic base conjugate nanoparticles for treating tumors and preparation method thereof
  • Amphiphilic base conjugate nanoparticles for treating tumors and preparation method thereof
  • Amphiphilic base conjugate nanoparticles for treating tumors and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Add raltitrexed (15 mg) and clofarabine (10 mg) into the sample bottle, then add 5 ml of dimethyl sulfoxide, and stir at room temperature for 12 hours to obtain the amphiphilic base conjugate. figure 1 is the chemical structural formula of the amphiphilic base conjugate (ratitrexed / clofarabine), and the amphiphilic base conjugate is formed by molecular recognition between raltitrexed and clofarabine . figure 2 One-dimensional NMR of the amphiphilic base conjugate (raltitrexed / clofarabine) 1 H NMR spectrum, test solvent is d 6 -DMSO. figure 2The assignment of the proton peaks in is as follows: δ(ppm from TMS), 8.14(1H, NCHCC), 7.84(1H, CONHCH), 7.59-7.61(2H, CCONHCNC, CCHCHCCCH), 7.36-7.40(3H, CCHCHCCCH, SCCHCHC) ,6.23(2H,NH 2 ), 5.91 (1H, SCCCHHC), 5.20 (1H, OCHCHCHCH), 5.11 (1H, OCHCHCHCH), 4.51 (2H, CCH 2 N), 4.33-4.36 (2H, OCHCHCHCH), 4.12, (1H, COHNCH), 4.0 (1H, CHCHOHCH), 3.74-3.81 (3H, CHCH 2 OH),2.98(3H,NCH 3 ),2.13(3H,CCH 3 ),1.84-1.98(4H,CHCH 2 CH 2...

Embodiment 2

[0038] Add doxifluridine (10 mg) and clofarabine (12 mg) into a sample bottle, then add 5 ml of dimethyl sulfoxide, stir at 40°C for 24 hours, and cool to room temperature to obtain the amphiphilic base base conjugates.

[0039] The chemical structural formula of the amphiphilic base conjugate synthesized in this embodiment is as follows Figure 4 shown. Doxifluridine and clofarabine form this amphiphilic base conjugate through molecular recognition between the bases.

[0040] The above-mentioned amphiphilic base conjugate (doxifluridine / clofarabine) was dissolved in dimethyl sulfoxide, dropped into water at room temperature, and then the dimethyl sulfoxide was removed to obtain two Aqueous solutions of nanoparticles of hydrophilic base conjugates. The transmission electron micrographs of the nanoparticles based on the amphiphilic base conjugate of doxifluridine and clofarabine prepared in this example are as follows: Figure 5 As shown, the average size of the nanoparticl...

Embodiment 3

[0042] Add bisfural fluorouracil (8 mg) and clofarabine (12 mg) into the sample bottle, then add 4 ml of dimethyl sulfoxide, stir at 60°C for 18 hours, cool to room temperature to obtain the amphiphilic base conjugate compound.

[0043] The chemical structural formula of the amphiphilic base conjugate synthesized in this embodiment is as follows Image 6 shown. The amphiphilic base conjugate is formed by the molecular recognition between bisfural fluorouracil and clofarabine.

[0044] Dissolve the prepared amphiphilic base conjugate (bisfururacil / clofarabine) in dimethyl sulfoxide, drop it into water at room temperature, and then remove the dimethyl sulfoxide to obtain amphiphilic Aqueous solutions of nanoparticles of sex base conjugates. The average size of the nanoparticles prepared in this example based on the amphiphilic base conjugate of bisfururacil / clofarabine is about 110 nanometers.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the technical field of biological medicine, in particular to amphiphilic basic group conjugate nanometer particles for treating tumors and a preparation method and application thereof. The amphiphilic basic group conjugate nanometer particles for treating tumors comprise amphiphilic basic group conjugates formed by connecting hydrophobic antitumor basic group similar drugs and hydrophilic antitumor basic group similar drugs through non covalent bonds. Compared with the prior art, the amphiphilic basic group conjugate nanometer particles can complete conveying of antitumor drugs independently, no substance of the nanometer size is needed to serve as a carrier, and the toxic or side effect caused by introduction of the carrier is avoided.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to an amphiphilic base conjugate nanoparticle for treating tumors and a preparation method and application thereof. Background technique [0002] Malignant tumor (cancer) has always been the main disease that causes the death rate of people all over the world to rise. Therefore, how to effectively treat malignant tumors has become one of the problems to be solved urgently in the world. At present, the treatment methods for malignant tumors mainly include the following: surgical resection, chemotherapy, radiation therapy, immune and biological therapy. Among them, chemotherapy is one of the most effective treatment methods. However, most antitumor drugs have the following disadvantages, such as poor solubility, poor stability, large toxic and side effects on normal tissues, and short blood residence time. In order to solve the above problems, a large number of literatures have...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/55A61K9/14A61K45/06A61P35/00
CPCA61K9/14A61K45/06
Inventor 朱新远颜德岳王大力
Owner SHANGHAI JIAOTONG UNIV