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Multifunctional nanosystem effectively reverses multidrug resistance in tumors

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P-glycoprotein (P-gp/ABCB1) is a typical type of multiple drug resistance (MDR) transport protein that can recognize and promote the drug efflux of tumor cells, severely limiting the efficacy of anti-tumor drugs.

BAY-1082439, a specific inhibitor against phosphatidylinositol-3-kinase (PI3K) 110α and 110β subunits, can reverse P-gp-mediated MDR by down-regulating P-gp expression. However, BAY-1082439 has shortcomings such as poor water solubility, short half-life, and high clearance rate in vivo.

A research group led by Prof. Chen Zhuo from the Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, has established a targeting drug delivery nano-system PBDF [P: poly(L-lactide-co-glycolide)-Thiol (PLGA-SH); B: BAY-1082439; D: doxorubicin (DOX); F: Folic acid-polyethylene glycol-Thiol (FA-PEG-SH)].

It comprises doxorubicin (DOX) and BAY-1082439 respectively encapsulated by biodegradable PLGA-SH nanoparticles (NPs) that are grafted to gold nanorods (Au NRs) modified with FA-PEG-SH, which can enhance the efficacy to reverse P-gp mediated MDR and to target tumor cells, and finally the efficiency to inhibit MDR tumors overexpressing P-gp. The study was published in Cancer Letters.

"Compared with free DOX combined with BAY-1082439, PBDF NPs significantly enhanced the uptake of DOX, improved the activity of reversing MDR, inhibited , and induced S-phase arrest and apoptosis of KB-C2 cells," said Prof. Chen.

The in vivo animal experiments further confirmed that PBDF NPs enhanced the anti-tumor ability of DOX and inhibited the development of KB-C2 tumors.

Besides, PBDF NPs inhibited the metastasis of KB-C2 cells in the liver and/or the lung of nude mice but had no obvious toxic effect on .

This study develops an achievable and applicable targeted therapy strategy for MDR tumors with high biocompatibility and the potential to inhibit MDR tumor progression and tumor metastasis.

More information: Ruikun Lin et al, A multi-functional nano-system combining PI3K-110α/β inhibitor overcomes P-glycoprotein mediated MDR and improves anti-cancer efficiency, Cancer Letters (2023). DOI: 10.1016/j.canlet.2023.216181

Journal information: Cancer Letters

Citation: Multifunctional nanosystem effectively reverses multidrug resistance in tumors (2023, May 12) retrieved 16 June 2024 from
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