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Long-circulating nanoparticle for targeting circulating tumor cells as well as preparation and application thereof

A technology of tumor cells and nanoparticles, which is applied in the field of long-circulation nanoparticles and its preparation and application, can solve the problems of inability to effectively utilize the specific recognition of polypeptides, and achieve improved drug bioavailability, good physiological compatibility, and encapsulation high rate effect

Active Publication Date: 2017-10-20
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after the preparation enters the body's circulation, it is easily recognized by the body's immune system, especially macrophages, and is quickly cleared out of the body. It is difficult to contact with circulating tumor cells and cannot effectively exert the effect of peptide-specific recognition.

Method used

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  • Long-circulating nanoparticle for targeting circulating tumor cells as well as preparation and application thereof
  • Long-circulating nanoparticle for targeting circulating tumor cells as well as preparation and application thereof
  • Long-circulating nanoparticle for targeting circulating tumor cells as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of DTX-SLNs-PepCD47

[0043] This embodiment provides the preparation method of SLNs as a control experiment, specifically as follows:

[0044]Weigh 3mg of DTX and 20mg of soybean lecithin into a vial, add 2mL of methanol to dissolve. Weighing 1 mg of SA-PepCD47 was dissolved in a small amount of dimethyl sulfoxide, and then mixed with the above methanol solution to obtain a mixed solution. At the same time, take 60 mg of glyceryl monostearate and melt it in a water bath at 70° C. to obtain a molten liquid. The above-mentioned mixed solution is mixed with the molten liquid to obtain a uniform oil phase, and then the water phase containing the emulsifier (preheated to 70°C) was quickly added to the oil phase, after dispersion, placed in an ultrasonic cell pulverizer for ultrasonication, stirred for 5 hours to evaporate the organic solvent, and DTX-SLNs-PepCD47 was obtained. Wherein, the emulsifier is Tween-80. The particle size, potential, drug l...

Embodiment 2

[0045] Example 2 Preparation of DTX-SLNs-Pep10

[0046] This embodiment provides the preparation method of SLNs as a control experiment, specifically as follows:

[0047] Weigh 3mg of DTX and 20mg of soybean lecithin into a vial, add 2mL of methanol to dissolve. Weighing 3 mg of SA-Pep10 was dissolved in a small amount of dimethyl sulfoxide, and then mixed with the above methanol solution to obtain a mixed solution. At the same time, take 60 mg of glyceryl monostearate and melt it in a water bath at 70° C. to obtain a molten liquid. The above-mentioned mixed solution is mixed with the molten liquid to obtain a uniform oil phase, and then the water phase containing the emulsifier (preheated to 70°C) was quickly added to the oil phase, after dispersion, placed in an ultrasonic cell pulverizer for ultrasonication, stirred for 5 hours to evaporate the organic solvent, and DTX-SLNs-Pep10 was obtained. Wherein, the emulsifier is Tween-80. The particle size, potential, drug loadin...

Embodiment 3

[0048] Example 3 Preparation of DTX-SLNs-PepCD47-Pep10

[0049] The preparation method of the long-circulating nanoparticles targeting circulating tumor cells of the present invention is as follows:

[0050] Weigh 3mg of DTX and 20mg of soybean lecithin into a vial, add 2mL of methanol to dissolve. 1 mg SA-PepCD47 and 3 mg SA-Pep10 were weighed and dissolved in a small amount of dimethyl sulfoxide, and then mixed with the above methanol solution to obtain a mixed solution. At the same time, 60 mg of glyceryl monostearate was weighed and melted in a water bath at 70° C. to obtain a molten liquid. The above-mentioned mixed solution is mixed with the molten liquid to obtain a uniform oil phase. The emulsifier was dispersed in purified water in a water bath at 70°C to prepare a water phase, wherein the emulsifier was Tween-80. Then, the aqueous phase (preheated to 70°C in advance) was quickly added to the oil phase, after dispersion, placed in an ultrasonic cell pulverizer for ...

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Abstract

The invention relates to a long-circulating nanoparticle for targeting circulating tumor cells. The long-circulating nanoparticle is prepared from chemical medicine, a solid lipid material and an emulsifier, wherein the surface of the nanoparticle is modified with macrophage phagocytosis-resistant polypeptide and circulating tumor cell targeting polypeptide. The invention also provides a preparation method of the long-circulating nanoparticle. The preparation method comprises the following steps of mixing the macrophage phagocytosis-resistant polypeptide, the circulating tumor cell targeting polypeptide, and an organic solvent dissolved with a chemical drug, and then mixing the melted solid lipid material, so as to obtain an oil phase; uniformly dispersing the emulsifier into water, so as to obtain a water phase; adding the oil phase into the water phase, and removing the organic solvent after the dispersing is uniform. The invention also provides application of the long-circulating nanoparticle in preparing a preparation for treating the circulating tumor cells. The long-circulating nanoparticle for targeting the circulating tumor cells has the advantages that the circulating tumor cells can be identified in the blood circulation in a targeting way, the phagocytosis of the macrophage is inhibited, the withering of the circulating tumor cells is caused by the chemical medicine, the tumor transfer process is disturbed, and the tumor transfer is obviously prohibited.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a long-circulating nanoparticle targeting circulating tumor cells and its preparation and application. Background technique [0002] Studies have found that tumors are mostly organ-confined diseases when they first occur, but eventually almost all of them spread to distant organs through the bloodstream to form metastasis, which is the main cause of death in cancer patients. The presence of circulating tumor cells in the peripheral blood of patients is a necessary prerequisite for tumor metastasis and recurrence. Circulating tumor cells mainly refer to tumor cells released into the peripheral blood circulation from solid tumors or metastases spontaneously or due to diagnostic and therapeutic operations, and complete hematogenous metastasis mainly through the following steps: separation from the primary tumor; infiltration into the vascular system; Survival in...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/337A61P35/00A61K31/704
CPCA61K31/337A61K31/704
Inventor 曹青日刘疆燕崔京浩
Owner SUZHOU UNIV
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