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A highly effective tumor targeting nanoprobe with a novel membrane penetration mechanism

创建时间:  2021/03/01  李晨晨   浏览次数:   

Efficient targeted tumor therapy has long been a major clinical challenge. Traditional targeting methods based on enhanced permeability and retention effect (EPR) have a targeting rate of only ≈5%.To solve this problem, a novel graphene-based tumor cell nucleus targeting fluorescent nanoprobe (GTTN) is a novel tumor targeting mechanism. GTTN is an amphiphilic fluorescent probe with graphene-like single crystal structure, and its periphery is functionalized by sulfonic acid and hydroxyl groups. The probe has the characteristic of targeting specific tumor cells by directly passing through the cell membrane and specifically targeting the tumor nucleus by taking advantage of changes in the permeability of tumor cell membrane in tumor tissues. This new targeting mechanism is called membrane permeability targeting (CMPT) mechanism, which is quite different from the EPR effect. These probes can identify tumor tissue at an early stage and track tumor cell invasion and metastasis at the single-cell level. The tumor targeting rate increased from less than 5% to more than 50%. The achievement of this efficient and accurate targeting of tumor cells will accelerate the arrival of a new era of cancer diagnosis and treatment.

We used CMPT mechanism to prepare a highly effective GTTN targeting tumor tissues. GTTN combined with CMPT can achieve a clear interface of tumor tissue in the early stage and track the metastasis and invasion of tumor cells at the single-cell level. CMPT is a novel tumor targeting mechanism that shows great potential in the targeting of nanoparticles/nanomedicines to tumor tissues, with high effectiveness and non-interference with normal tissues and cells. This strategy paints a bright blueprint for cancer treatment and diagnosis. Further research is needed to accurately quantify the parameters, further study the roles and effects of all physical and chemical parameters throughout the target process, and generate detailed standard design specifications to engineer the CMPT mechanism. Following this design principle, nanoparticles/nanomedicines can accurately target tumor nuclei in vivo with minimal uptake from normal tissues. With the development of materials science and synthetic biology, the precise manufacture of nanoparticles/nanomedicines based on design principles has become a reality. CMPT has a promising future in the field of cancer therapy.

https://doi.org/10.1002/adma.201807456

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