A preparation method of folate receptor-targeted substrate-loaded nano-microbubbles

A folic acid receptor and carrier technology, applied in the field of drug active protective agent, targeted drug carrier synthesis, can solve the problems of hindering the application of photodynamic therapy, unable to guarantee activity, low specificity, etc., and achieve easy penetration of tissues and cell membranes , to ensure biological activity and stability, no biological toxicity effect

Active Publication Date: 2020-12-29
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the substrate is easily degraded quickly after entering the body, and the activity cannot be guaranteed
[0005] In addition, the targeting of photodynamic therapy in liver cancer is also a problem that needs to be solved urgently. Since the existing photodynamic therapy rarely involves research on deep tissues such as the liver, it can be applied to other superficial tissues based on photodynamic therapy. The sensitivity mainly depends on the passive targeting effect of the retention effect of the photosensitizer on the tumor tissue, as well as the targeted irradiation of the manipulated light source.
This passive targeting with low specificity can easily cause damage to normal tissues, which hinders the further application of photodynamic therapy. Therefore, how to ensure the targeting of substrates is also a difficult problem.

Method used

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  • A preparation method of folate receptor-targeted substrate-loaded nano-microbubbles

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Effect test

Embodiment 1

[0032] see figure 1 As shown, the present invention provides a folic acid receptor-targeted substrate-loaded nano-microbubble, the substrate-loaded nano-microbubble is composed of a core template and a shell, and the core template is CdSe / ZnS quantum dot-coelenterofluorescence Coelenterazine complex and / or coelenterazine, when the core template contains CdSe / ZnS quantum dot-coelenterazine complex, the CdSe / ZnS quantum dot-coelenterazine complex consists of CdSe / ZnS quantum dot-coelenterazine complex The dots are covalently coupled with luciferin; the shell is a folic acid cross-linked polyethylene glycol poly(lactic-co-glycolic acid) polymer.

[0033] Using CdSe / ZnS quantum dots coupled with coelenterazine fluorescein, CdSe / ZnS quantum dots can play a role in converting wavelengths, absorbing blue light with a wavelength of about 450-480nm and immediately converting it into red light at about 650nm, that is, Bioluminescence Resonance Energy Transfer. .

[0034] The present ...

Embodiment 1

[0036] The invention provides a method for preparing substrate-loaded nano-microbubbles targeting folic acid receptors. In the preparation of the substrate-loaded nano-microbubbles, the method has the advantages of stable encapsulation efficiency, uniform particle size, high yield, and easy synthesis and processing. The advantage of the method is simple, it comprises the following steps:

[0037] S1: preparing the folic acid cross-linked polyethylene glycol poly(lactic-co-glycolic acid) polymer and making it form the shell;

[0038] S2: when the core template is coelenterazine, loading the core template into the shell to complete the preparation of the substrate-loaded nano-microbubbles;

[0039] When the core template is a CdSe / ZnS quantum dot-coelenterazine complex, the CdSe / ZnS quantum dot-coelenterazine complex is prepared and made to form the core template, and the core template is loading into the shell to complete the preparation of the substrate-loaded nano-microbubbl...

Embodiment 2

[0042] The difference between this example and Example 1 of the preparation method is that in step S1, polylactic acid / glycolic acid (50:50, denoted as PLGA-COOH) with a molecular weight of 25KD and carboxyl groups on the surface is used as the carrier for the outer shell, and diamino Polyethylene glycol (molecular weight is 3.5KD, recorded as NH 2 -PEG-NH 2 ) as the linker, and folic acid (denoted as FA) as the specific targeting ligand. Folate-targeted polyethylene glycol-polylactic acid / glycolic acid polymer (denoted as PLGA-PEG-FA) was prepared by a five-step process:

[0043] Step 1: Synthesis of PLGA-NHS: PLGA-COOH and N-hydroxysuccinimide (denoted as NHS) are coupled to activate the carboxyl group.

[0044] Dissolve 0.04MM PLGA-COOH in 4ml dichloromethane, dissolve 0.4MM NHS and 0.3MM dicyclohexylcarbodiimide in 2ml dichloromethane, mix them, and place them in a shaker at a slow speed Shake well overnight, add 80ml ice methanol and ether mixed solution (the volume ra...

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Abstract

The invention discloses a folate receptor-targeted substrate-loaded nano-microbubble. The substrate-loaded nano-microbubble is composed of a core template and a shell, and the core template is a CdSe / ZnS quantum dot-coelenterazine complex and / or or coelenterazine; the outer shell is folic acid cross-linked polyethylene glycol poly(lactic-co-glycolic acid) polymer. The invention also discloses a preparation method of the substrate-loaded nano microbubble. The substrate-loaded nano-microbubble of the present invention has the advantages of targeted release, delayed degradation, and maintaining the activity of the CdSe / ZnS quantum dot-coelenterazine complex and / or coelenterazine in vivo.

Description

technical field [0001] The invention relates to the field of drug activity protective agents and the field of synthesis of targeted drug carriers, in particular to a folic acid receptor-targeted substrate-carrying nano-microbubble and a preparation method thereof. Background technique [0002] Photodynamic therapy (Photodynamic Therapy, PDT) is a new method to treat tumors after surgery, chemotherapy and radiotherapy. Good therapeutic effects have been achieved in superficial tissue tumors such as skin cancer and breast cancer. At present, photodynamic therapy mainly uses a laser emitter as an external light source to excite a photosensitizer (Photosensitizer, PS) that is injected intravenously and distributed in the tumor tissue, thereby triggering a photodynamic reaction (Photodaynamic Reaction, PDR) to generate a cytotoxic agent - reactive oxygen species (Reactive Oxygen Species). Oxygen Species, ROS), leading to necrosis and / or apoptosis of tumor cells, and destroying n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K38/44A61K47/55A61K47/54A61K41/00A61P35/00
CPCA61K9/5146A61K38/44A61K41/0052C12Y113/12007A61K2300/00
Inventor 王立宇程翔宋祥铭李加欢周星郑启昌
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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