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叶酸偶联 δ-戊内酯-聚乙二醇的三嵌段共聚物作为一种有前途的载药体系，用于靶向阿霉素递送。

Folic acid conjugated δ-valerolactone-poly(ethylene glycol) based triblock copolymer as a promising carrier for targeted doxorubicin delivery.

机构信息

Chemical Biology, Rajiv Gandhi Centre for Biotechnology, Poojappura, Kerala, India.

出版信息

PLoS One. 2013 Aug 21;8(8):e70697. doi: 10.1371/journal.pone.0070697. eCollection 2013.

DOI:10.1371/journal.pone.0070697
PMID:23990912
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3749165/
Abstract

The aim of this study is to test the hypothesis that the newly synthesized poly(δ-valerolactone)/poly(ethylene glycol)/poly(δ-valerolactone) (VEV) copolymer grafted with folic acid would impart targetability and further enhance the anti-tumor efficacy of doxorubicin (DOX). Here, folic acid conjugated VEV (VEV-FOL) was synthesized by a modified esterification method and characterized using IR and NMR. DOX loaded VEV-FOL micelles were synthesized using a novel solvent evaporation method and were obtained with a mean diameter of 97 nm with high encapsulation efficiency and sustained in vitro release profile. Comparative studies of polymer micelles with and without folate for cellular uptake and cytotoxicity were done on folate receptor-positive breast cancer cell line, MDAMB231. The intracellular uptake tests showed significant increase in folate micellar uptake when compared to non-folate-mediated micelles. MTT assay followed by apoptosis assays clearly indicated that folate decorated micelles showed significantly better cytotoxicity (IC50 = 0.014 µM) and efficiency to induce apoptosis than other treated groups. Moreover, a significant G2/M arrest was induced by DOX loaded VEV-FOL micelles at a concentration where free drug failed to show any activity. Thus, our results show that the folic acid-labeled VEV copolymer is a promising biomaterial with controlled and sustainable tumor targeting ability for anticancer drugs which can open new frontiers in the area of targeted chemotherapy.

摘要

本研究旨在验证以下假设

即新合成的聚（δ-戊内酯）/聚乙二醇/聚（δ-戊内酯）（VEV）共聚物接枝叶酸后将赋予靶向性，并进一步增强阿霉素（DOX）的抗肿瘤功效。在此，通过改良的酯化法合成了叶酸接枝的 VEV（VEV-FOL），并通过 IR 和 NMR 进行了表征。采用新型溶剂蒸发法合成了 DOX 负载的 VEV-FOL 胶束，平均粒径为 97nm，包封效率高，体外释放呈持续状态。对叶酸受体阳性乳腺癌细胞系 MDAMB231 进行了载药聚合物胶束与非叶酸介导的聚合物胶束的细胞摄取和细胞毒性的比较研究。细胞内摄取实验表明，与非叶酸介导的胶束相比，叶酸介导的胶束摄取显著增加。MTT 法和凋亡实验清楚地表明，叶酸修饰的胶束比其他处理组具有更好的细胞毒性（IC50=0.014µM）和诱导凋亡的效率。此外，DOX 负载的 VEV-FOL 胶束在浓度下诱导显著的 G2/M 期阻滞，而游离药物在此浓度下没有显示出任何活性。因此，我们的结果表明，叶酸标记的 VEV 共聚物是一种有前途的生物材料，具有可控和可持续的肿瘤靶向能力，可为抗癌药物开辟新的前沿，为靶向化疗领域开辟新的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/4c445cd1208c/pone.0070697.g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/f4c4dc01c02e/pone.0070697.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/a44391df4e2d/pone.0070697.g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/1f2fc8523af7/pone.0070697.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/f16ee186e781/pone.0070697.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/e5a1c48e59ad/pone.0070697.g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/89b15e5f47ed/pone.0070697.g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/4c445cd1208c/pone.0070697.g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/f4c4dc01c02e/pone.0070697.g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/ec514f237c59/pone.0070697.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/6c8ee6c313bc/pone.0070697.g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/1f2fc8523af7/pone.0070697.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/f16ee186e781/pone.0070697.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/e5a1c48e59ad/pone.0070697.g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/89b15e5f47ed/pone.0070697.g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de08/3749165/4c445cd1208c/pone.0070697.g010.jpg

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