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Targeted drug-bearing ultrasonic microbubble and preparation method thereof

A technology of ultrasonic microbubbles and drug loading, which can be used in pharmaceutical formulations, echo/ultrasonic imaging agents, anti-tumor drugs, etc., and can solve the problem of poor targeting of drug-loaded microbubbles

Inactive Publication Date: 2011-08-03
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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Problems solved by technology

[0004] Although ultrasound-mediated targeted drug-loaded microbubbles have the advantages of safety, high efficiency, and strong controllability, and have initially shown broad application prospects, the traditional ultrasound-mediated targeted drug-loaded microbubbles are not very targeted. To enhance its targeting, further modification is required

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  • Targeted drug-bearing ultrasonic microbubble and preparation method thereof
  • Targeted drug-bearing ultrasonic microbubble and preparation method thereof
  • Targeted drug-bearing ultrasonic microbubble and preparation method thereof

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Embodiment Construction

[0038] The targeted drug-loaded ultrasonic microbubbles and their preparation methods will be further described in detail below mainly in conjunction with the accompanying drawings and specific examples.

[0039] One embodiment of targeted drug-loaded ultrasonic microbubbles includes: a lipid bilayer shell, a targeting polypeptide fixed outside the lipid bilayer shell, a biologically inert gas wrapped inside the lipid bilayer shell, and a dispersed Drug particles in a lipid bilayer shell.

[0040] The targeting polypeptide is a polypeptide or protein derivative comprising the amino acid sequence CGNKRTRGC (LyP-1 polypeptide). Biotin is attached to the targeting polypeptide, so that the targeting polypeptide and the lipid bilayer shell can be connected through a biotin-avidin-biotin bridge or a biotin-streptavidin-biotin bridge.

[0041] The lipid bilayer shell of this embodiment is a phospholipid or a phospholipid derivative, such as 1,2-dipalmitoyl-sn-glyceryl-3-phosphatidic...

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Abstract

The invention relates to a targeted drug-bearing ultrasonic microbubble comprising a lipide dimolecular layer outer shell, targeted polypeptide fixed at the outer side of the lipide dimolecular layer outer shell, a biological inert gas wrapped in the lipide dimolecular layer outer shell and medicament granules dispersed in the lipide dimolecular layer outer shell. The targeted polypeptide is a polypeptide or protein derivative containing an amino acid sequence CGNKRTRGC. By connecting the polypeptide or protein derivative containing a tumor targeted peptide sequence outside the lipide dimolecular layer outer shell, the obtained targeted drug-bearing ultrasonic microbubble can target the lymph vessels and the tumor cells of a tumor, can detect and diagnose the generation, the development and the curative effect on the tumor in real time through high-frequency ultrasonic imaging and can crush the microbubble through low-frequency ultrasound to release the medicament granules so as to achieve the aim of controllably and targetedly releasing the medicament, thereby having extremely important meanings to the prevention, diagnose and treatment of the tumor. In addition, the invention also relates to a preparation method of the targeted drug-bearing ultrasonic microbubble.

Description

【Technical field】 [0001] The invention relates to the technical field of ultrasonic microbubble development, in particular to a targeted drug-loaded ultrasonic microbubble and a preparation method thereof. 【Background technique】 [0002] In 1968, Gramiak first reported the small bubbles that can enhance the imaging, that is, ultrasonic microbubble contrast agent (UCA). The emergence of UCA has created a new field of non-invasive ultrasound diagnosis and treatment. With the deepening of its research, it is found that ultrasound microbubble contrast agent is not only a good contrast agent for ultrasound imaging, but also an important drug delivery carrier. Research on ultrasound microbubble contrast agents carrying genes or drug-targeted therapy is becoming more and more extensive in the medical field. Ultrasound microbubble contrast agent-targeted therapy includes ultrasound-mediated drug-loaded microbubble therapy and ultrasound-mediated targeted drug-loaded microbubble th...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/42A61K31/337A61K48/00A61K49/22A61P35/00
Inventor 严飞郑海荣李翔靳巧锋
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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