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Double-targeting drug-loaded microbubble as well as preparation method and application thereof

A dual-targeting, drug-carrying technology, applied in the field of biomedicine, can solve the problems that hinder the chemotherapy drug paclitaxel, and achieve the effect of improving the efficacy of tumor treatment, increasing the concentration, and increasing the permeability

Active Publication Date: 2022-07-12
PEKING UNIV THIRD HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above methods did not solve the problem that the massive proliferation of stroma in the microenvironment of pancreatic cancer would hinder the chemotherapy drug paclitaxel from entering tumor cells

Method used

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  • Double-targeting drug-loaded microbubble as well as preparation method and application thereof
  • Double-targeting drug-loaded microbubble as well as preparation method and application thereof
  • Double-targeting drug-loaded microbubble as well as preparation method and application thereof

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preparation example Construction

[0038] The present invention also provides the preparation method of the dual-targeted drug-loaded microbubbles described in the above technical solution, comprising the following steps:

[0039] (1) Distearoylphosphatidylcholine, distearoylphosphatidylethanolamine-polyethylene glycol 2000, distearoylphosphatidylethanolamine-polyethylene glycol-cyclic RGD peptide, distearoylphospholipid Acetylethanolamine-polyethylene glycol-cyclic CLT1 peptide and paclitaxel were dissolved in chloroform solution to obtain mixed solution A;

[0040] (2) after the mixed solution A is spin-dried, dry overnight in a vacuum drying oven to obtain the film B;

[0041] (3) Dissolving film B in phosphate buffer with pH=7.4, heating to 50°C, and hydrating for 1 hour to form transparent liquid C;

[0042] (4) ultrasonicating the transparent liquid C in a water bath for 5 minutes, and then ultrasonicating the probe for 1 minute to homogenize it;

[0043] (5) After the ultrasonic probe is finished, resp...

Embodiment 1

[0049] Preparation of 1.59-micron dual-targeting microbubbles:

[0050] Step 1. Distearoylphosphatidylcholine, distearoylphosphatidylethanolamine-polyethylene glycol 2000, distearoylphosphatidylethanolamine-polyethylene glycol-cyclic RGD peptide, distearoylphospholipid Acetylethanolamine-polyethylene glycol-cyclic CLT1 peptide and paclitaxel were dissolved in chloroform solution to obtain mixed solution A;

[0051] Step 2, spin-dried the mixed solution A and dry it in a vacuum drying oven for eight hours to obtain the film B;

[0052] Step 3. Dissolve film B in pH=7.4 phosphate buffer and heat to 50°C for hydration, and hydrate for one hour to form clear solution C;

[0053] Step 4. After the transparent liquid C is subjected to water bath ultrasound for 5 minutes, the probe ultrasound is performed for another minute to homogenize it;

[0054] Step 5. After the probe is sonicated, add propylene glycol and glycerol to the above solution according to the volume ratio of 1:1:8 ...

Embodiment 2

[0058] Preparation of 1.59-micron dual-targeting microbubbles:

[0059] Step 1. Distearoylphosphatidylcholine, distearoylphosphatidylethanolamine-polyethylene glycol 2000, distearoylphosphatidylethanolamine-polyethylene glycol-cyclic RGD peptide, distearoylphospholipid Acetylethanolamine-polyethylene glycol-cyclic CLT1 peptide and paclitaxel were dissolved in chloroform solution to obtain mixed solution A;

[0060] Step 2, spin-dried the mixed solution A and dry it in a vacuum drying oven for eight hours to obtain the film B;

[0061] Step 3. Dissolve film B in pH=7.4 phosphate buffer and heat to 50°C for hydration, and hydrate for one hour to form clear solution C;

[0062] Step 4. After the transparent liquid C is subjected to water bath ultrasound for 5 minutes, the probe ultrasound is performed for another minute to homogenize it;

[0063] Step 5. After the probe is sonicated, add propylene glycol and glycerol to the above solution in a volume ratio of 1:1:8 to form mixe...

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Abstract

The invention provides a dual-targeting drug-loaded microbubble as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The double-targeting drug-loading microbubble provided by the invention comprises a shell layer and an inner core, the shell layer is a lipid monomolecular layer modified by a double-targeting ligand, and the lipid monomolecular layer modified by the double-targeting ligand carries a chemotherapeutic drug paclitaxel. And the component of the inner core is inert gas. The double-targeting drug-loaded microbubble provided by the invention can target a tumor site, and the accumulation amount of a chemotherapeutic drug paclitaxel at the tumor site is increased so as to improve the chemotherapeutic effect.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a dual-targeted drug-carrying microbubble and a preparation method and application thereof. Background technique [0002] At present, chemotherapy is still the main way to treat pancreatic cancer, but because the chemotherapy drug paclitaxel cannot be delivered to the tumor site, there are still problems of poor efficacy and large systemic side effects of chemotherapy. However, a chemotherapeutic drug paclitaxel delivery system (Nat Rev Clin Oncol 2016, 13(12), 750-765) developed based on nanotechnology was found to be useful for increasing the targeted delivery of chemotherapeutic drug paclitaxel, so it can be used as an increase in chemotherapeutic drug paclitaxel Targeted delivery has been a novel strategy to improve the efficacy of chemotherapy. [0003] In preclinical research or clinical research, microbubbles, as a micron-sized chemotherapy drug paclitaxel delivery sy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/337A61K41/00A61K47/62A61K47/24A61P35/00
CPCA61K9/5031A61K9/5015A61K9/5089A61K41/0028A61K31/337A61K47/62A61P35/00A61K2300/00
Inventor 葛辉玉张路路梁晓龙崔立刚陈文曾兰马久祎汤清双孙利红
Owner PEKING UNIV THIRD HOSPITAL