期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 93, 期 -, 页码 90-96出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2016.08.014
关键词
Paclitaxel nanocrystals; Polyelectrolytes; Surface modification; Cell internalization; Cell cytotoxicity
资金
- MOE [2009-0093815]
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Korea government, MSIP [2015R1A2A1A10051596]
In this study, we investigated the influence of paclitaxel nanocrystals (PTX-NC) surface charge on cell internalization and cell cytotoxicity. PTX-NCs were prepared using the nano-precipitation method. The surface-modified PTX-NCs were prepared using an absorption method with positively charged poly(allylamine hydrochloride) (PAH) and negatively charged poly(sodium 4-styrenesulfonate) (PSS). The morphologies of the surface-modified and unmodified PTX-NCs were characterized by field emission scanning electron microscopy. An in vitro drug release study was performed in phosphate-buffered saline (pH 7.4) containing 0.5% (w/v) Tween 80 for 48 h. Cell internalization was evaluated at time intervals of 0.5, 1, and 2 h, and cell cytotoxicity was analyzed for 24 h using A549 cells. Three different types of PTX-NCs with a mean size of around 300-400 nm were successfully prepared. The zeta-potential revealed PSS-PTX-NCs (-22.7 +/- 5.1 mV), PTX-NCs (-2.4 +/- 2.9 mV), and PAH-PTX-NCs (+19.3 +/- 3.4 mV). The three types of PTX-NC exhibited higher drug release than pure PTX. The positive charge on PTX-NC resulted in higher cell uptake and cell cytotoxicity than the negative charge on PTX-NC. Moreover, the positive charge on PTX-NC showed stronger interactions with bovine serum albumin. In conclusion, the positive charge on PTX-NCs improved cell internalization, cell cytotoxicity, and interactions with bovine serum albumin. (C) 2016 Elsevier B.V. All rights reserved.
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