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新型聚乙二醇化胆甾醇体用于将非瑟酮靶向乳腺癌：体外评价和体内抗肿瘤研究。

Novel PEGylated cholephytosomes for targeting fisetin to breast cancer: in vitro appraisal and in vivo antitumoral studies.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

Head of International Publication and Nanotechnology Center INCC, Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University of Alexandria, Alexandria, Egypt.

出版信息

Drug Deliv Transl Res. 2024 Feb;14(2):433-454. doi: 10.1007/s13346-023-01409-5. Epub 2023 Aug 30.

DOI:10.1007/s13346-023-01409-5
PMID:37644299
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10761494/
Abstract

Fisetin (FIS) is a multifunctional bioactive flavanol that has been recently exploited as anticancer drug against various cancers including breast cancer. However, its poor aqueous solubility has constrained its clinical application. In the current work, fisetin is complexed for the first time with soy phosphatidylcholine in the presence of cholesterol to form a novel biocompatible phytosomal system entitled "cholephytosomes." To improve fisetin antitumor activity against breast cancer, stearylamine bearing cationic cholephytosomes (mPHY) were prepared and furtherly modified with hyaluronic acid (HPHY) to allow their orientation to cancer cells through their surface exposed phosphatidylserine and CD-44 receptors, respectively. In vitro characterization studies revealed promising physicochemical properties of both modified vesicles (mPHY and HPHY) including excellent FIS complexation efficiency (˷100%), improved octanol/water solubility along with a sustained drug release over 24 h. In vitro cell line studies against MDA-MB-231 cell line showed about 10- and 3.5-fold inhibition in IC50 of modified vesicles compared with free drug and conventional drug-phospholipid complex, respectively. Preclinical studies revealed that both modified cholephytosomes (mPHY and HPHY) had comparable cytotoxicity that is significantly surpassing free drug cytotoxicity. TGF-β1and its non-canonical related signaling pathway; ERK1/2, NF-κB, and MMP-9 were involved in halting tumorigenesis. Thus, tailoring novel phytosomal nanosystems for FIS could open opportunity for its clinical utility against cancer.

摘要

漆黄素（FIS）是一种多功能生物活性黄烷醇，最近已被开发为抗癌药物，可用于治疗多种癌症，包括乳腺癌。然而，其较差的水溶性限制了其临床应用。在目前的工作中，漆黄素首次与大豆卵磷脂在胆固醇存在下形成一种新型的生物相容性植物甾醇体系统，命名为“胆甾醇体”。为了提高漆黄素对乳腺癌的抗肿瘤活性，制备了带有正电荷的胆甾醇体（mPHY）的硬脂胺，并进一步用透明质酸（HPHY）进行修饰，使它们能够通过表面暴露的磷脂酰丝氨酸和 CD-44 受体分别靶向癌细胞。体外特性研究揭示了两种修饰囊泡（mPHY 和 HPHY）具有有前途的物理化学性质，包括优异的 FIS 包合效率（˷100%）、改善的辛醇/水溶解度以及 24 小时以上的药物持续释放。体外细胞系研究表明，与游离药物和常规药物-磷脂复合物相比，修饰囊泡的 IC50 分别约降低了 10 倍和 3.5 倍。临床前研究表明，两种修饰的胆甾醇体（mPHY 和 HPHY）具有相当的细胞毒性，明显超过游离药物的细胞毒性。TGF-β1及其非经典相关信号通路；ERK1/2、NF-κB 和 MMP-9 参与阻止肿瘤发生。因此，为 FIS 定制新型植物甾醇纳米系统为其在癌症治疗中的临床应用提供了机会。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/42cd5a156157/13346_2023_1409_Fig11_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/7fa74eefac9a/13346_2023_1409_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/62a980c6ab1b/13346_2023_1409_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/d366a6fbf2e4/13346_2023_1409_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/755cad1f4ee8/13346_2023_1409_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/3d17d55b9d8d/13346_2023_1409_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/29e95b2a26e7/13346_2023_1409_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/1a9db6da0a09/13346_2023_1409_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/76ccd7349561/13346_2023_1409_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/166f/10761494/7aa160e8556b/13346_2023_1409_Fig10_HTML.jpg
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