Radiosensitizer and preparation method thereof

A technology of sensitizer and water solvent, which is applied in the field of radiotherapy sensitizer and its preparation, can solve the problems of limited improvement of siRNA stability, no risk of viral vectors, failure to meet clinical safety and long-term effect, etc. Achieve the effects of reducing radiosensitivity, stable properties, and easy administration

Inactive Publication Date: 2015-03-18
汪步海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing modification methods have very limited improvement on the stability of siRNA
Therefore, siRNA connected with traditional non-viral vectors cannot meet the needs of clinical safety and long-term effect; while chemically modified siRNA is mostly modified with lipophilic

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A radiotherapy sensitizer, comprising: 80% PLGA-PEI / hypericin nano-micelle, 8% HIF-1α-siRNA, 12% hyaluronic acid, wherein the molecular weight of hyaluronic acid is 11000 . Its preparation process comprises the following steps:

[0030] 1. Weigh 0.2g of Poloxamer 188, dissolve in 10mL of deionized water, and wait to dissolve.

[0031] 2. PEI-acetone stock solution: Weigh 0.2g of polyetherimide (PEI) with a molecular weight of 25,000, Tween 800.05g, a little acetone, dissolve it by ultrasonic and pour it into a 10mL volumetric flask, then add acetone dropwise to volume.

[0032] 3. Weigh 0.2g of PLGA with a molecular weight of 10000, 0.1g of Tween 80, 1mL of PEI-acetone stock solution, 6.5mL of acetone, and 2.5mL of dichloromethane, and ultrasonically dissolve them.

[0033] 4. Dissolve hypericin in ethanol solvent to prepare a 2.5 mg / mL solution.

[0034] 5. Take 40 μL of the hypericin solution prepared in step 4, mix with 10 mL of the poloxamer 188 solution prepared...

Embodiment 2

[0041] A radiotherapy sensitizer, comprising: 50% PLGA-PEI / hypericin nano-micelle, 5% HIF-1α-siRNA, 45% hyaluronic acid, wherein the molecular weight of hyaluronic acid is 6600 . Its preparation process comprises the following steps:

[0042] 1. Weigh 0.2 g of polyvinylpyrrolidone (PVA), and add it gradually into 10 mL of physiological saline under magnetic stirring to obtain a clear PVA solution.

[0043] 2. PEI-acetone stock solution: Weigh 0.2g of polyetherimide (PEI) with a molecular weight of 25,000, Tween 800.05g, a little acetone, dissolve it by ultrasonic and pour it into a 10mL volumetric flask, then add acetone dropwise to volume.

[0044] 3. Weigh 0.2g of PLGA with a molecular weight of 10000, 0.1g of Tween 80, 1mL of PEI-acetone stock solution, 6.5mL of acetone, and 2.5mL of dichloromethane, and ultrasonically dissolve them.

[0045] 4. Dissolve hypericin in ethanol solvent to prepare a 2.5 mg / mL solution.

[0046] 5. Take 40 μL of the hypericin solution prepare...

Embodiment 3

[0053] A radiotherapy sensitizer, comprising: 80% PLGA-PEI / hypericin nano-colloids, 8% HIF-1α-siRNA, 33% hyaluronic acid, wherein the molecular weight of hyaluronic acid is 800 . Its preparation process comprises the following steps:

[0054] 1. Weigh 0.2g of Poloxamer 188, dissolve in 10mL of deionized water, and wait to dissolve.

[0055] 2. PEI-acetone stock solution: Weigh 0.2g of polyetherimide (PEI) with a molecular weight of 25,000, Tween 800.05g, a little acetone, dissolve it by ultrasonic and pour it into a 10mL volumetric flask, then add acetone dropwise to volume.

[0056] 3. Weigh 0.2g of PLGA with a molecular weight of 10000, 0.1g of Tween 80, 1mL of PEI-acetone stock solution, 6.5mL of acetone, and 2.5mL of dichloromethane, and ultrasonically dissolve them.

[0057] 4. Dissolve hypericin in ethanol solvent to prepare a 2.5 mg / mL solution.

[0058] 5. Take 40 μL of the hypericin solution prepared in step 4, mix with 10 mL of the poloxamer 188 solution prepared ...

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Abstract

The invention relates to a radiosensitizer and a preparation method thereof, and the radiosensitizer can improve a radiation resistance problem of solid tumors; the radiosensitizer comprises 50%-80% of PLGA-PEI/hypericin nano colloidal particles, 5%-8% of HIF-1alpha-siRNA, and 12%-45% of hyaluronic acid, wherein the hyaluronic acid molecular weight can be any one of 11000, 6600 and 800. The preparation method comprises the steps of firstly preparing the PLGA-PEI/hypericin nano colloidal particles by an emulsion solvent evaporation method, then dropwise adding the HIF-1alpha-siRNA, and finally wrapping with HA. The preparation process is simple and easy to implement.

Description

technical field [0001] The invention relates to a radiotherapy sensitizer and a preparation method thereof, in particular to a pharmaceutical preparation capable of improving the radiation resistance of solid tumors and a preparation method thereof. Background technique [0002] Radiation therapy is one of the important methods in the treatment of malignant tumors. There are many factors affecting the curative effect of radiotherapy, such as the sensitivity of tumor cells to radiation, cell cycle, and the existence of tumor stem cells. In clinical practice, it has been found that the hypoxia of tumor cells is the main reason for radiation resistance and poor clinical efficacy. Conventional radiation doses cannot effectively kill these cells and become the root cause of tumor recurrence and metastasis. Existing radiosensitizers cannot directly reach hypoxic cells, and even if they do, they will be cleared quickly, and cannot maintain sufficient concentration and long time in...

Claims

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Application Information

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IPC IPC(8): A61K48/00A61K31/7052A61K47/36A61K47/34A61P35/00A61K31/122
Inventor 汪步海张立英张俊玲王晓磊
Owner 汪步海
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