期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 513, 期 1-2, 页码 543-553出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2016.09.067
关键词
Paclitaxel; Nanocrystals; Herceptin; HER2-positve breast cancer; Tumor-targeting
资金
- Korea Healthcare Technology RD Project
- Ministry for Health & Welfare Affairs, Republic of Korea [HI12C0529]
- National Research Foundation of Korea (NRF) grant by the Korean Government (MSIP) [2009-0083538]
The objective of this study was to prepare Herceptin (HCT)-functionalized paclitaxel nanocrystals and evaluated their cell-specific interactions, cellular accumulation, and growth inhibition in HER2-positve breast cancer cells as a tumor-targeted delivery module. Paclitaxel (PTX) was fabricated in the form of nanocrystals (PNCs) by a sono-precipitation method, and HCT were coated using a facile non-covalent method (PNCs-HCT). Our results showed that the PNCs-HCT were stable for at least 1 month at 4 degrees C with no noticeable desorption of HCT. The release test showed that PNCs-HCT exhibited sustained drug release similar to only PNCs but with a higher release rate than only PTX powder. Cellular uptake, cytotoxicity, and cell cycle arrest studies revealed that PNCs-HCT exhibit greater binding affinity and higher cell-specific internalization to HER2-positive breast cancer cell lines as compared to PNCs, followed by enhanced cell growth inhibition. HCT-functionalized PNCs presented in this study offer a promising strategy for targeted pure drug nanocrystal delivery and enhancing the efficiency of anticancer therapy. (C) 2016 Elsevier B.V. All rights reserved.
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