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Tumor targeting haematoporphyrin injection for ultrasonic therapy and preparation method thereof

A porphyrin injection and tumor targeting technology, which is applied in the field of tumor-targeted hematoporphyrin injection for ultrasound therapy and its preparation, and can solve the problems of harsh clinical use conditions, low water solubility of hematoporphyrin, low tumor targeting, etc. problems, to achieve the effect of reducing photosensitivity toxicity, prolonging residence time, and wide application potential

Inactive Publication Date: 2017-07-07
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Aiming at the problems of low water solubility of hematoporphyrin, low tumor targeting, strong phototoxicity and harsh clinical conditions, the present invention provides a tumor-targeted hematoporphyrin injection for ultrasonic therapy, which can effectively carry The drug reaches the tumor site, combined with in vitro ultrasound conditions, improves the therapeutic effect of hematoporphyrin and reduces its phototoxicity

Method used

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  • Tumor targeting haematoporphyrin injection for ultrasonic therapy and preparation method thereof
  • Tumor targeting haematoporphyrin injection for ultrasonic therapy and preparation method thereof
  • Tumor targeting haematoporphyrin injection for ultrasonic therapy and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0023] Step 1, dissolve folic acid in N,N dimethylformamide, add N-hydroxysuccinimide and N,N'dicyclohexylcarbodiimide, stir and react at 5°C for 0.5h, then add amino Cyclodextrin continued to react for 12 hours, wherein the molar ratio of folic acid, N-hydroxysuccinimide, N,N'dicyclohexylcarbodiimide, and aminocyclodextrin was [1:1:1:10];

[0024] Step 2, the reaction solution obtained in step 1 is spun to dryness to obtain a dried product, which is dissolved in water and then filtered to obtain a clarified filtrate. After the spun-dried and clarified filtrate, the dried product is dissolved in acetone, and the filter cake is redissolved after filtration. In acetone, filter to obtain a filter cake, which is dried to obtain folic acid-coupled cyclodextrin;

[0025] Step 3, mix the folic acid-coupled cyclodextrin and hematoporphyrin obtained in step 2, dissolve them in water, and stir in the dark for 12 hours at 5°C, wherein the molar ratio of folic acid-coupled cyclodextrin an...

Embodiment 2

[0029] Step 1, dissolve folic acid in N,N dimethylformamide, add N-hydroxysuccinimide and N,N'dicyclohexylcarbodiimide, stir and react at 30°C for 2h, then add amino ring Dextrin continued to react for 24 hours, wherein the molar ratio of folic acid, N-hydroxysuccinimide, N,N'dicyclohexylcarbodiimide, and aminocyclodextrin was [5:1:1:10];

[0030] Step 2, the reaction solution obtained in step 1 is spun to dryness to obtain a dried product, which is dissolved in water and then filtered to obtain a clarified filtrate. After the spun-dried and clarified filtrate, the dried product is dissolved in acetone, and the filter cake is redissolved after filtration. In acetone, filter to obtain a filter cake, which is dried to obtain folic acid-coupled cyclodextrin;

[0031] Step 3, mix the folic acid-coupled cyclodextrin and hematoporphyrin obtained in step 2, dissolve them in water, and stir for 48 hours at 25° C. in the dark, where the molar ratio of folic acid-coupled cyclodextrin an...

Embodiment 3

[0035] Step 1, dissolve folic acid in N,N dimethylformamide, add N-hydroxysuccinimide and N,N'dicyclohexylcarbodiimide, stir and react at 50°C for 5h, then add amino ring Dextrin continued to react for 48 hours, wherein the molar ratio of folic acid, N-hydroxysuccinimide, N,N'dicyclohexylcarbodiimide, and aminocyclodextrin was [10:1:1:10];

[0036] Step 2, the reaction solution obtained in step 1 is spun to dryness to obtain a dried product, which is dissolved in water and then filtered to obtain a clarified filtrate. After the spun-dried and clarified filtrate, the dried product is dissolved in acetone, and the filter cake is redissolved after filtration. In acetone, filter to obtain a filter cake, which is dried to obtain folic acid-coupled cyclodextrin;

[0037]Step 3, mix the folic acid-coupled cyclodextrin and hematoporphyrin obtained in step 2, dissolve them in water, and stir for 96 hours in the dark at 50°C, wherein the molar ratio of folic acid-coupled cyclodextrin an...

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Abstract

The invention discloses a tumor targeting haematoporphyrin injection for ultrasonic therapy and a preparation method thereof. The preparation method comprises the following steps of firstly, enabling folate and aminocyclodextrin to react to generate folate-conjugated cyclodextrin; enabling the folate-conjugated cyclodextrin and haematoporphyrin to react, so as to obtain a folate-conjugated cyclodextrin haematoporphyrin inclusion compound; finally, adding the folate-conjugated cyclodextrin haematoporphyrin inclusion compound and acetone chloroform into injection water, and sterilizing, so as to obtain the tumor targeting haematoporphyrin injection for the ultrasonic therapy. The tumor targeting haematoporphyrin injection for ultrasonic therapy has the advantages that after the tumor targeting haematoporphyrin injection is injected into a tumor-bearing mice body, the in-vitro ultrasonic therapy is adopted, so that the targeting property of the haematoporphyrin for high expression ofexpressing the malicious tumor tissues in a folate receptor is obviously improved, the retention time of the drug in the tumor part is prolonged, and the tumor therapy effect is improved; the light stability of the haematoporphyrin is improved, the photosensitive toxic and side reaction of light sensitizing of the haematoporphyrin is decreased, and the wide application potential is realized in clinical application.

Description

technical field [0001] The invention relates to a tumor-targeted hematoporphyrin injection for ultrasonic therapy and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Photodynamic therapy (PDT) is a new method of treating tumor diseases with photosensitizing drugs and laser activation. The use of specific wavelengths to irradiate tumor sites can activate photosensitizing drugs selectively gathered in tumor tissues, triggering photochemical reactions to destroy tumors. Hematoporphyrin is a photosensitive substance, which can undergo energy state transition and emit characteristic fluorescence under light stimulation, and at the same time transfer part of the energy to surrounding oxygen to generate highly active singlet oxygen. Singlet oxygen can oxidize with nearby biomacromolecules to produce cytotoxicity and kill tumor cells. Because hematoporphyrin is very sensitive to light, oxidants and some rays, the storage and...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/69A61K9/08A61K47/22A61K31/409A61P35/00
CPCA61K41/0033A61K9/0019A61K9/08A61K31/409A61K47/22
Inventor 杜富强王传金吴娇吴禹茜
Owner NANJING UNIV OF SCI & TECH
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