Folate receptor medium, optical excitation photosensitive drug conjugate and preparation method of optical excitation photosensitive drug conjugate

A technology of photosensitive drugs and folic acid receptors, which is applied in drug combinations, pharmaceutical formulations, photodynamic therapy, etc., can solve the problems that have not been reported in the literature of targeted photosensitive drug conjugates, achieve enhanced effects, prolong circulation time, Avoid the effect of devouring

Inactive Publication Date: 2019-04-05
衍全生物科技(太仓)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] So far, there have been no literature reports on this kind o

Method used

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  • Folate receptor medium, optical excitation photosensitive drug conjugate and preparation method of optical excitation photosensitive drug conjugate
  • Folate receptor medium, optical excitation photosensitive drug conjugate and preparation method of optical excitation photosensitive drug conjugate
  • Folate receptor medium, optical excitation photosensitive drug conjugate and preparation method of optical excitation photosensitive drug conjugate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of folic acid-polyethylene glycol-hematoporphyrin conjugate, and synthesis of folic acid-polyethylene glycol-photosensitive coupling agent.

[0022] 1) Synthesis of polyethylene glycol for the function of folic acid.

[0023] Weigh the double-end amino polyethylene glycol (NH 2 -PEG-NH 2 , M=3200Da) 640mg was dissolved in 10ml anhydrous DMSO, 2ml DMSO solution dissolved with folic acid FA and NHS was added, then DCC, TEA (molar dosage of each substance NH) were added in turn 2 -PEG-NH 2 : FA: NHS: DCC: TEA = 1: 1: 1.5: 1.5: 5), under nitrogen protection, stirred at room temperature, and reacted in the dark for 12 h, the reaction mixture was diluted with 20 ml of deionized water, and centrifuged at 500 rpm to remove the secondary The product dicyclohexylurea was added with 10 ml of acetone to remove unreacted folic acid. The supernatant was put into a dialysis tube with a molecular weight cut-off of 3000 Da, diluted with deionized water for 48 ho...

Embodiment 2

[0026] Example 2 Observation of phototoxic side effects and targeting effect in tumor tissue.

[0027] 1) Phototoxicity side reaction test

[0028] Take hematoporphyrin injection (Chongqing Huading Now Biopharmaceutical Co., Ltd.) as a comparative example. Twenty ICR mice, half male and half male, were randomly divided into 2 groups with 10 mice in each group. The mice in each group were given the medicines of the examples and comparative examples through the tail vein (the dosage calculated according to hematoporphyrin was 6.26 × 10). -2 g·Kg -1 ·d -1 ). Before administration, the backs of the mice were dehaired, and the dehaired area was 2cm×2cm. 1h after administration, the two groups of mice were placed under the light condition of 5500K color temperature light source (approximately outdoor afternoon sunlight) 3500LX for 20min, and the back skin of the mice was used as the main observation area, and the comparative examples and pairs were observed at different times. ...

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Abstract

The invention belongs to the technical filed of polymer drugs, and particularly relates to a folate receptor medium, an optical excitation photosensitive drug conjugate and a preparation method of theoptical excitation photosensitive drug conjugate. The preparation method comprises the steps: firstly, folate and amino polyethylene glycol are subjected to an amidation reaction and then subjected to an amidation reaction together with haematoporphyrin HPD, and the polyethylene glycol flexible chain conjugate with folate receptor targeted optical excitation haematoporphyrin genes is obtained. The conjugate prepared through the method can target a tumour cell through the folate receptor medium and enters the cell through endocytosis to accelerate accumulation of the haematoporphyrin in the tumour cell, and through irradiating by purple light or red light with the specific wavelength, accurate diagnosis and treatment can be carried out; and meanwhile, a simple and effective way is providedfor preparing the targeted haematoporphyrin fluorescent molecular drug conjugate.

Description

technical field [0001] The invention belongs to the technical field of polymer drugs, and in particular relates to a folate receptor-mediated, light-excited photosensitizing drug conjugate and a preparation method thereof. Background technique [0002] Light-excited hematoporphyrin photosensitive drugs are a new class of drugs for cancer diagnosis and treatment. They can excite fluorescence through violet light irradiation, and can be used for early diagnosis of cancer through fluorescence detection. It can also treat cancer through photodynamic therapy, and its treatment is much better than the three traditional methods of surgery, radiotherapy and chemotherapy. Small. The reason is that 1 hour after this hematoporphyrin drug is injected into the body, the radioactive content in each tissue reaches a peak, and the tissue distribution order is lung>liver>kidney>blood>stomach>intestine>spleen>heart>muscle>thymus>brain>bone, tumor. The conten...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/60A61K41/00A61K49/00A61P35/00
CPCA61K41/0042A61K41/0071A61K41/008A61K49/0036
Inventor 叶衍铭邹志杨叶莹朱行倩
Owner 衍全生物科技(太仓)有限公司
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