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一种新型的基于甜茶苷的溶解度增强型胶束用于增强癌症治疗。

A Novel Solubility-Enhanced Rubusoside-Based Micelles for Increased Cancer Therapy.

作者信息

Zhang Meiying, Dai Tongcheng, Feng Nianping

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai, 201203, China.

Department of Pharmaceutics, School of Pharmacy, Key Laboratory of Smart Drug Delivery, Ministry of Education, Fudan University, Shanghai, 201203, China.

出版信息

Nanoscale Res Lett. 2017 Dec;12(1):274. doi: 10.1186/s11671-017-2054-4. Epub 2017 Apr 13.

DOI:10.1186/s11671-017-2054-4
PMID:28410552
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5391341/
Abstract

Many anti-cancer drugs have a common problem of poor solubility. Increasing the solubility of the drugs is very important for its clinical applications. In the present study, we revealed that the solubility of insoluble drugs was significantly enhanced by adding rubusoside (RUB). Further, it was demonstrated that RUB could form micelles, which was well characterized by Langmuir monolayer investigation, transmission electron microscopy, atomic-force microscopy, and cryogenic transmission electron microscopy. The RUB micelles were ellipsoid with the horizontal distance of ~25 nm and vertical distance of ~1.2 nm. Insoluble synergistic anti-cancer drugs including curcumin and resveratrol were loaded in RUB to form anti-cancer micelles RUB/CUR + RES. MTT assay showed that RUB/CUR + RES micelles had more significant toxicity on MCF-7 cells compared to RUB/CUR micelles + RUB/RES micelles. More importantly, it was confirmed that RUB could load other two insoluble drugs together for remarkably enhanced anti-cancer effect compared to that of RUB/one drug + RUB/another drug. Overall, we concluded that RUB-based micelles could efficiently load insoluble drugs for enhanced anti-cancer effect.

摘要

许多抗癌药物都存在溶解度差的常见问题。提高药物的溶解度对其临床应用非常重要。在本研究中，我们发现通过添加甜茶苷（RUB）可显著提高难溶性药物的溶解度。此外，还证明RUB可形成胶束，通过朗缪尔单分子层研究、透射电子显微镜、原子力显微镜和低温透射电子显微镜对其进行了很好的表征。RUB胶束呈椭圆形，水平距离约为25 nm，垂直距离约为1.2 nm。将包括姜黄素和白藜芦醇在内的难溶性协同抗癌药物负载于RUB中，形成抗癌胶束RUB/CUR + RES。MTT分析表明，与RUB/CUR胶束+ RUB/RES胶束相比，RUB/CUR + RES胶束对MCF-7细胞具有更显著的毒性。更重要的是，已证实与RUB/一种药物+ RUB/另一种药物相比，RUB可同时负载其他两种难溶性药物以显著增强抗癌效果。总体而言，我们得出结论，基于RUB的胶束可有效负载难溶性药物以增强抗癌效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/591db2528c89/11671_2017_2054_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/4de824a6914a/11671_2017_2054_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/5a868619a7fd/11671_2017_2054_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/03c69ee71d77/11671_2017_2054_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/af610451c1c5/11671_2017_2054_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/d10c6d870bb6/11671_2017_2054_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/46e6fbd85173/11671_2017_2054_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/591db2528c89/11671_2017_2054_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/4de824a6914a/11671_2017_2054_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/5a868619a7fd/11671_2017_2054_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/03c69ee71d77/11671_2017_2054_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/af610451c1c5/11671_2017_2054_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/d10c6d870bb6/11671_2017_2054_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/46e6fbd85173/11671_2017_2054_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a63/5391341/591db2528c89/11671_2017_2054_Fig7_HTML.jpg

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