ATP (adenosine triphosphate) sensitive fluorescent probe lipidosome with tumor targeting and tracing effects, and preparation method and application thereof

Abstract

The invention relates to an ATP (adenosine triphosphate) sensitive fluorescent probe lipidosome, which is characterized in that ATP sensitive nucleotide double chains are encapsulated in a lipid bimolecular layer membrane coupled with tumor targeting polypeptide to form a nanometer vesicle; the ATP sensitive nucleotide double chains are formed by self assembly of an ATP sensitive nucleotide single chain coupled with fluorescent dye and an ATP sensitive nucleotide complementary single chain coupled with a fluorescent quenching agent according to the base complementation and pairing principle; the lipid bimolecular layer membrane coupled with the tumor targeting polypeptide consists of tumor targeting polypeptide coupled pegylation phosphatidyl ethanolamine, phospholipid and cholesterol according to a mole ratio being (2-8):(42-78):(20-50). The invention also provides a preparation method of the lipidosome. The fluorescent probe lipidosome has the tumor active targeting, ATP sensitive intelligent fluorescent light opening and in vivo long circulation functions; the preparation process is simple.

Description

technical field [0001] The invention belongs to the field of imaging reagents, in particular to a fluorescent probe liposome. Background technique [0002] Tumor has become a major disease that threatens human health. At present, when the tumor is diagnosed, the vast majority of cancer patients are in the middle and advanced stages, and the treatment methods mainly include surgery, radiotherapy, and chemotherapy. However, patients with advanced tumors are prone to recurrence, drug resistance, metastasis and complications after treatment, which are the main reasons for treatment failure and patient death. Therefore, it is of great significance to carry out early diagnosis of tumors to improve the treatment effect and reduce the mortality of cancer patients. Fluorescent tracer technology refers to the introduction of fluorescent substances into the cells or tissues to be tracked or developed, and the use of fluorescent properties to provide information about the researched o...

AI Technical Summary

Problems solved by technology

As a fluorescent probe, the micelles can be effectively delivered in vivo, enter cells, and have a high signal-low background ratio, excellent selectivity and biocompatibility, but there are the following problems: 1. Only rely on the enhanced penetration of nanometer size and The retention (EPR) effect reaches the tumor site, without active targeting, and the targeting efficiency is poor. The article does not provide in vivo targeting experiment data; 2. The PEG chain is too short to achieve the effect of prolonging the internal circulation; 3. It is necessary to synthesize oligo-containing Hybrid molecules of nucleotides, polyethylene glycol and di-fatty acyl lipids, with many synthetic steps, difficult synthesis and complex purification operations

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