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Preparation method of tumor-targeting nanoparticle carrier co-loaded with breast cancer chemotherapy drug mtdh siRNA

A chemotherapeutic drug and nanoparticle technology, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and drug combinations, etc., can solve the problems of inability to penetrate cell membranes, short half-life of siRNA, and prolong the circulation time. , Improve the curative effect, reduce the effect of toxic and side effects

Active Publication Date: 2021-02-19
宋振川
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Naked siRNA has an extremely short half-life due to the action of nucleases in plasma
Moreover, due to high molecular weight, hydrophilicity, and high charge density, naked siRNA can hardly penetrate cell membranes

Method used

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  • Preparation method of tumor-targeting nanoparticle carrier co-loaded with breast cancer chemotherapy drug mtdh siRNA
  • Preparation method of tumor-targeting nanoparticle carrier co-loaded with breast cancer chemotherapy drug mtdh siRNA
  • Preparation method of tumor-targeting nanoparticle carrier co-loaded with breast cancer chemotherapy drug mtdh siRNA

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] a. After dissolving 18mg polyethyleneimine-lactic acid glycolic acid polymer in 1ml dichloromethane, add 0.2ml deionized water and mix well;

[0027] b. Ultrasonic crush the above solution and emulsify it into a homogeneous emulsion; use the cell disruptor at 25% power for 5 minutes;

[0028] c. After mixing 1.8ml of vinyl alcohol with a mass concentration of 1.8% and 0.2ml of hydrophobic paclitaxel with a mass concentration of 1.8% and 2-4ml of dichloromethane, add it to the above-mentioned emulsion, and then continuously add 10ml of it with a mass concentration of 0.6%. In the state of vinyl alcohol, it was ultrasonically crushed again and then emulsified into a homogeneous emulsion;

[0029] d. After the organic phase in the emulsion prepared in step c is removed with a low-pressure rotary evaporator, the nanoparticle cores loaded with paclitaxel are obtained;

[0030] e. Rinse the paclitaxel-loaded nanoparticle core with deionized water for 5 minutes at 12,000 rpm,...

Embodiment 2

[0037] Embodiment 2: the difference between this embodiment and embodiment 1 is that

[0038] a. After dissolving 20mg polyethyleneimine-lactic acid glycolic acid polymer in 1ml dichloromethane, add 0.25ml deionized water and mix well;

[0039] b. Ultrasonic crush the above solution and emulsify it into a homogeneous emulsion; use the cell disruptor at 25% power for 5 minutes;

[0040] c. After mixing 2.0ml of vinyl alcohol with a mass concentration of 2.0% and 0.25ml of hydrophobic paclitaxel with a mass concentration of 2.0% and 2-4ml of dichloromethane, add it to the above emulsion, and then continuously add 10ml of it with a mass concentration of 0.6%. In the state of vinyl alcohol, it was ultrasonically crushed again and then emulsified into a homogeneous emulsion;

[0041] d. After the organic phase in the emulsion prepared in step c is removed with a low-pressure rotary evaporator, the nanoparticle cores loaded with paclitaxel are obtained;

[0042] e. Rinse the pacli...

Embodiment 3

[0043] Embodiment 3: the difference between this embodiment and embodiment 1 is,

[0044] a. After dissolving 22mg polyethyleneimine-lactic acid glycolic acid polymer in 1ml dichloromethane, add 0.3ml deionized water and mix well;

[0045] b. Ultrasonic crush the above solution and emulsify it into a homogeneous emulsion; use the cell disruptor at 25% power for 5 minutes;

[0046] c. After mixing 1.8-2.2ml of vinyl alcohol with a mass concentration of 2.2% and 0.3ml of hydrophobic paclitaxel with a mass concentration of 2.2% and 2-4ml of dichloromethane, add it to the above-mentioned emulsion, and then continuously add 10ml of it with a mass concentration of In the state of 0.6% vinyl alcohol, it was ultrasonically crushed again and then emulsified into a homogeneous emulsion;

[0047] d. After the organic phase in the emulsion prepared in step c is removed with a low-pressure rotary evaporator, the nanoparticle cores loaded with paclitaxel are obtained;

[0048] e. Rinse th...

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Abstract

The invention discloses a preparation method of a tumor-targeting nanoparticle carrier co-loaded with breast cancer chemotherapy drug MTDH siRNA, which comprises dissolving polyethyleneimine-lactic acid glycolic acid polymer in dichloromethane, adding deionized water, then ultrasonically crush the above solution and emulsify it into a homogeneous emulsion, mix vinyl alcohol and hydrophobic paclitaxel with dichloromethane, add the above emulsion, then ultrasonically crush and emulsify, evaporate the emulsion to obtain a suspension of nanoparticles, and then mix the nanoparticles After preparing the paclitaxel-loaded nanoparticle core from the suspension, rinse, stir and centrifuge. The invention can simultaneously carry breast cancer chemotherapeutic drugs and nucleic acid into breast cancer tumor cells with high expression of MTDH gene, inhibit cell proliferation, and has remarkable tumor targeting in vivo and in vitro. The anti-tumor effect of the invention is clear, and the carrier material used has high biological safety, good biocompatibility, biodegradability, non-toxicity and no immunogenicity. The preparation process is simple, easy to operate, saves time and energy, and is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of nano-medicines, and in particular relates to a preparation method of tumor-targeting nano-particles co-carrying breast cancer chemotherapeutic drug MTDH siRNA. [0002] technical background [0003] Malignant tumor is an important disease that threatens human health and social development. Its occurrence is a complex process of multi-gene and multi-factor interaction, which eventually leads to abnormal cell proliferation and death. Breast cancer has become the tumor with the highest incidence rate in women, and as a highly heterogeneous tumor, breast cancer has significant differences in pathological typing, molecular typing, and prognosis. Although estrogen receptor-positive breast cancer can benefit from endocrine therapy, chemotherapy still plays an important role in postoperative systemic treatment and treatment of recurrence and metastasis. However, triple-negative breast cancer is highly invasive, prone to re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/337A61K31/713A61P35/00
CPCA61K31/337A61K31/713A61K2300/00
Inventor 宋振川
Owner 宋振川
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