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用于黄酮类化合物抗癌治疗的基于普朗尼克的药物递送系统

Pluronics-Based Drug Delivery Systems for Flavonoids Anticancer Treatment.

作者信息

Ronka Sylwia, Kowalczyk Aleksandra, Baczyńska Dagmara, Żołnierczyk Anna K

机构信息

Department of Polymer Engineering and Technology, Faculty of Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.

Department of Molecular and Cellular Biology, Faculty of Pharmacy with Division of Laboratory Diagnostics, Wrocław Medical University, Borowska 211A, 50-556 Wrocław, Poland.

出版信息

Gels. 2023 Feb 8;9(2):143. doi: 10.3390/gels9020143.

Abstract

This research concerns the investigation of the preparation of polymeric nanocarriers containing a flavonoid-naringenin, xanthohumol or isoxanthohumol-based on Pluronics by the thin-film formation method. The size of the formed micelles and their stability upon dilution were evaluated using Dynamic light scattering (DLS) analysis; the high values of the drug loading and the encapsulation efficiency confirmed that the proposed systems of flavonoids delivery consisting of Pluronic P123 and F127 nanomicelles could effectively distribute the drug into tumour tissues, which makes these nanocarriers ideal candidates for passive targeting of cancer cells by the enhanced permeation and retention (EPR) effect. The in vitro cytotoxicity of proposed flavonoids in the Pluronic formulations was investigated by the SRB assay with human colon cancer cells. We designed mixed polymeric micelles, which was a successful drug delivery system for the case of naringenin not being able to enhance the bioavailability and cytotoxic activity of xanthohumol and isoxanthohumol. Furthermore, it was observed that the higher amount of polymer in the formulation achieved better cytotoxic activity.

摘要

本研究涉及基于普朗尼克通过薄膜形成法制备含黄酮类化合物(柚皮素、黄腐酚或异黄腐酚)的聚合物纳米载体。使用动态光散射(DLS)分析评估所形成胶束的尺寸及其稀释稳定性;高载药量和包封率证实,由普朗尼克P123和F127纳米胶束组成的所提出的黄酮类化合物递送系统可有效将药物分布到肿瘤组织中,这使得这些纳米载体成为通过增强渗透和滞留(EPR)效应被动靶向癌细胞的理想候选物。通过SRB法对人结肠癌细胞研究了普朗尼克制剂中所提出的黄酮类化合物的体外细胞毒性。我们设计了混合聚合物胶束,对于柚皮素无法提高黄腐酚和异黄腐酚的生物利用度和细胞毒性活性的情况而言,这是一种成功的药物递送系统。此外,观察到制剂中聚合物含量越高,细胞毒性活性越好。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/01bb/9957264/20037f89dd52/gels-09-00143-g001.jpg

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