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纳米结构脂质载体负载的磷脂-右布洛芬缀合物的抗癌活性

Anticancer Activity of Phospholipid-Dexibuprofen Conjugates Loaded in Nanostructured Lipid Carriers.

作者信息

Thiruchenthooran Vaikunthavasan, Świtalska Marta, Maciejewska Gabriela, Palko-Łabuz Anna, Bonilla-Vidal Lorena, Espina Marta, Luisa Garcia Maria, Wietrzyk Joanna, Souto Eliana B, Sánchez-López Elena, Gliszczyńska Anna

机构信息

Department of Food Chemistry and Biocatalysis, Wrocław University of Environmental and Life Sciences, Wrocław, Poland.

Department of Experimental Oncology, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland.

出版信息

Int J Nanomedicine. 2025 May 30;20:6999-7019. doi: 10.2147/IJN.S512505. eCollection 2025.

DOI:10.2147/IJN.S512505
PMID:40470113
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12134470/
Abstract

PURPOSE

In our work, we focused on the development of nanostructured lipid carriers (NLCs) loaded with dexibuprofen (DXI) and their application for cancer therapy by proposing the binding of phospholipids with this non-steroidal anti-inflammatory drug (NSAID) to obtain new delivery systems.

METHODS

We successfully synthesized seven conjugates with good yields, four of which are new, and have not been previously published in the literature. The structures of the obtained conjugates were confirmed and comparative in vitro studies of their antiproliferative activity were conducted, along with molecular modeling to assess their therapeutic potential.

RESULTS

1-DXI-2-hydroxy--glycero-3-phosphocholine (DXI-LPC), 1-DXI-2-oleoyl--glycero-3-phosphocholine (DXI-OA-PC) and 1-oleoyl-2-DXI--glycero-3-phosphocholine (OA-DXI-PC) showed selectivity for cancer cells, influencing the cell cycle and inducing apoptosis. Encapsulation of heterosubstituted conjugates with increased lipophilic character in NLC resulted in DXI-PA-PC-NLC and DXI-OA-PC-NLC with favorable size (around 150 nm) and polydispersity index of 0.15, high encapsulation efficacy (above 99%), long-term stability, and modified release profile (51.4% and 48.9% of DXI released from DXI-PA-PC-NLC and DXI-OA-PC-NLC, respectively). Antiproliferative assays confirmed enhanced activity of synthesized products and their increased accumulation in cancer cells.

CONCLUSION

This study describes the synthesis of new conjugates of DXI and phospholipids and their nanotechnological formulations for potential use in cancer therapy.

摘要

目的

在我们的工作中，我们专注于开发负载右布洛芬（DXI）的纳米结构脂质载体（NLCs），并通过提出磷脂与这种非甾体抗炎药（NSAID）的结合以获得新的递送系统，将其应用于癌症治疗。

方法

我们成功合成了七种产率良好的共轭物，其中四种是新的，此前未在文献中发表过。对所获得的共轭物的结构进行了确认，并对其抗增殖活性进行了体外比较研究，同时进行了分子建模以评估其治疗潜力。

结果

1 - DXI - 2 - 羟基 - 甘油 - 3 - 磷酸胆碱（DXI - LPC）、1 - DXI - 2 - 油酰基 - 甘油 - 3 - 磷酸胆碱（DXI - OA - PC）和1 - 油酰基 - 2 - DXI - 甘油 - 3 - 磷酸胆碱（OA - DXI - PC）对癌细胞具有选择性，影响细胞周期并诱导凋亡。将具有增加亲脂性的杂取代共轭物封装在NLC中，得到了尺寸适宜（约150 nm）、多分散指数为0.15、包封率高（超过99%）、长期稳定性好且释放曲线得到改善的DXI - PA - PC - NLC和DXI - OA - PC - NLC（分别从DXI - PA - PC - NLC和DXI - OA - PC - NLC中释放出51.4%和48.9%的DXI）。抗增殖试验证实了合成产物的活性增强及其在癌细胞中的积累增加。

结论

本研究描述了DXI与磷脂的新共轭物的合成及其用于癌症治疗潜在用途的纳米技术制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/e50c1180b992/IJN-20-6999-g0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/f150ac88f5cd/IJN-20-6999-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/4f803619e7fb/IJN-20-6999-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/de978251a66f/IJN-20-6999-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/6961dca48396/IJN-20-6999-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/f54ac2d9b073/IJN-20-6999-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/5e11cf0f70c7/IJN-20-6999-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/d3c814139177/IJN-20-6999-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/e50c1180b992/IJN-20-6999-g0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/f150ac88f5cd/IJN-20-6999-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/4f803619e7fb/IJN-20-6999-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/de978251a66f/IJN-20-6999-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/6961dca48396/IJN-20-6999-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/f54ac2d9b073/IJN-20-6999-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/5e11cf0f70c7/IJN-20-6999-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/d3c814139177/IJN-20-6999-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1fa/12134470/e50c1180b992/IJN-20-6999-g0008.jpg

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