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聚(3-羟基丁酸酯-CO-3-羟基戊酸酯) PHBHV 生物相容性纳米载体用于靶向结直肠癌的 5-FU 递送。

Poly(3-hydroxybutyrate-CO-3-hydroxyvalerate) PHBHV biocompatible nanocarriers for 5-FU delivery targeting colorectal cancer.

机构信息

a Advanced Polymer Materials Group , University Politehnica of Bucharest , Bucharest , Romania.

b Department of Biochemistry and Molecular Biology , University of Bucharest , Bucharest , Romania.

出版信息

Drug Deliv. 2019 Dec;26(1):318-327. doi: 10.1080/10717544.2019.1582729.

Abstract

Aiming to address the issue of poor bioavailability of most anti-tumor medicines against colorectal cancer, we developed a targeted anticancer nanocarrier using biocarriers able to both bind and easily release their load in a controlled manner. Poly(3-hydroxybutyrate-co-3-hydroxyvalerate) carriers were obtained via the emulsification-diffusion method, loaded with 5-fluorouracil and then characterized in terms of particle morphology and size (SEM, DLS), drug uptake and release. The cytotoxic potential of the 5-fluorouracil-loaded polymer nanocarriers on human adenocarcinoma cells (HT-29 cell line) was investigated. The in vitro studies clearly demonstrated that while the nanocarriers themselves slightly alter HT-29 cell viability, when loaded with 5-fluorouracil they significantly decrease cell viability, suggesting that the polymer itself exhibits low cytotoxicity and the drug-loaded carrier acts in an efficient manner to kill HT-29 human adenocarcinoma cells.

摘要

为了解决大多数针对结直肠癌的抗肿瘤药物生物利用度差的问题,我们开发了一种使用生物载体的靶向抗癌纳米载体,该载体能够以受控的方式结合并轻松释放其负载物。通过乳化扩散法获得聚(3-羟基丁酸酯-co-3-羟基戊酸酯)载体,负载 5-氟尿嘧啶,然后从颗粒形态和大小(SEM、DLS)、药物摄取和释放方面进行表征。研究了载有 5-氟尿嘧啶的聚合物纳米载体对人腺癌细胞(HT-29 细胞系)的细胞毒性潜力。体外研究清楚地表明,虽然纳米载体本身对 HT-29 细胞活力略有影响,但负载 5-氟尿嘧啶后,它们显著降低了细胞活力,这表明聚合物本身具有低细胞毒性,载药载体能够有效地杀死 HT-29 人腺癌细胞。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a697/6442118/4e5364d2d95b/IDRD_A_1582729_F0001_C.jpg

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