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A kind of medicine for treating tumor and preparation method thereof

A tumor treatment and drug technology, applied in the field of tumor treatment drugs and its preparation, can solve the problems of poor curative effect of tumor treatment, shortened triplet lifetime, etc., and achieve the effects of increasing toxicity, prolonging the circulation time in the body, and improving stability

Inactive Publication Date: 2018-06-05
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the internal heavy atom effect often leads to a significant shortening of the lifetime of the excited triplet state, which inhibits the increase in the quantum yield of singlet oxygen, which makes its tumor treatment effect poor.

Method used

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  • A kind of medicine for treating tumor and preparation method thereof
  • A kind of medicine for treating tumor and preparation method thereof
  • A kind of medicine for treating tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A drug for tumor treatment, comprising a nano-drug carrier and a photosensitizer loaded on the nano-drug carrier, the mass ratio of the photosensitizer to the nano-drug carrier is 2:1, and the nano-drug carrier is PEG-modified and heavy atom substituted Graphene quantum dots, whose general formula is PEG-I-GQDs, GQDs are graphene quantum dots with a thickness of 2-7nm, the photosensitizer is Ce6, and PEG is a linear PEG with a number average molecular weight of 16,000 containing an amino terminal group. The formula is as follows:

[0055] n takes a positive integer.

[0056] The preparation method of the above-mentioned medicine for tumor treatment, comprising the following steps:

[0057] (1) In the phosphate buffer solution of pH=7.5 that is dissolved with graphene quantum dots, add NaI and chloramine T, in the phosphate buffer solution, the concentration of graphene quantum dots is 0.02M, the added graphene quantum dots , The mass ratio of NaI and chloramine T is...

Embodiment 2

[0063] A drug for tumor treatment, comprising a nano-drug carrier and a photosensitizer loaded on the nano-drug carrier, the mass ratio of the photosensitizer to the nano-drug carrier is 3:1, and the nano-drug carrier is modified by PEG and replaced by heavy atoms Graphene quantum dots, whose general formula is PEG-Br-GQDs, GQDs are graphene quantum dots with a thickness of 2-7nm, the photosensitizer is ZnPc, and PEG is a linear PEG with a number average molecular weight of 30,000 containing two terminal amino groups. The general formula is as follows:

[0064] n takes a positive integer.

[0065] The preparation method of the above-mentioned medicine for tumor treatment, comprising the following steps:

[0066] (1) In the phosphate buffer solution of pH=8 that is dissolved with graphene quantum dot, add NaBr and chloramine T, in the phosphate buffer solution, the concentration of graphene quantum dot is 0.02M, the graphene quantum dot added , the mass ratio of NaBr and ch...

Embodiment 3

[0070] A drug for tumor treatment, comprising a nano-drug carrier and a photosensitizer loaded on the nano-drug carrier, the mass ratio of the photosensitizer to the nano-drug carrier is 0.5:1, and the nano-drug carrier is PEG-modified and heavy atom substituted Graphene quantum dots, whose general formula is PEG-I-GQDs, GQDs are graphene quantum dots with a thickness of 2-7nm, the photosensitizer is HA, and PEG is a linear PEG with a number average molecular weight of 2000 containing a hydroxyl group. The general formula is as follows:

[0071] n takes a positive integer.

[0072] The preparation method of the above-mentioned medicine for tumor treatment, comprising the following steps:

[0073] (1) In the phosphate buffer solution of pH=7 that is dissolved with graphene quantum dot, add NaI and chloramine T, in phosphate buffer solution, the concentration of graphene quantum dot is 0.02M, the added graphene quantum dot , the mass ratio of NaI and chloramine T is 1:2.5:2....

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Abstract

The invention relates to a drug for treating tumors and a preparation method thereof. The drug comprises a nanometer drug carrier and a photosensitizer carried by the nanometer drug carrier. A mass ratio of the photosensitizer to the nanometer drug carrier is (0.5-3): 1. The nanometer drug carrier is a graphene quantum dot subjected to PEG modification and heavy atom replacement and has a general formula of PEG-X-GQDs, wherein X represents a heavy atom and GQDs represents a graphene quantum dot. The preparation method comprises 1, adding heavy atom sodium salt and chloramine T into a phosphate buffer solution with the graphene quantum dot, carrying out stirring for a reaction, and then carrying out separation to obtain the heavy atom-substituted graphene quantum dot, 2, adding PEG and EDC / NHS into the aqueous solution of the heavy atom-substituted graphene quantum dot for a reaction, and carrying out separation purification to obtain PEG-X-GQDs, and 3, adding a DMSO solution of the photosensitizer into the PEG-X-GQDs aqueous solution, carrying out stirring for a reaction and carrying out separation to obtain a desired product. Compared with the existing tumor treatment drug, the drug provided by the invention has the advantages of strong targeting, photolytic activity and tumor tissue killing effects.

Description

technical field [0001] The invention relates to the field of photodynamic therapy, in particular to a medicine for tumor treatment and a preparation method thereof. Background technique [0002] Photodynamic therapy (Photodynamic Therapy, PDT) is a kind of singlet oxygen ( 1 o 2 ) and (or) free radicals, killing tumors or other pathological hyperplastic tissues to achieve a new type of medical technology for the treatment of cancer. The photosensitizer is the core of PDT, and the therapeutic effect of PDT depends directly on the retention of the photosensitizer in tumor cells and its singlet oxygen production rate under light. The introduction of nano-drug carriers can greatly improve the hydrophilicity and bioavailability of the photosensitizer, but at the same time, due to the excessive concentration of the photosensitizer in the local area, the probability of non-radiative transition from the excited state to the ground state is increased, making the singlet oxygen Yie...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/12A61P35/00
Inventor 任天斌吴志勇李艳董海青李永勇
Owner TONGJI UNIV
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