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Issue 8, 2015
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The aspect ratio effect of drug nanocrystals on cellular internalization efficiency, uptake mechanisms, and in vitro and in vivo anticancer efficiencies

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Abstract

In this paper, we investigated the aspect ratio (AR) effect of anticancer drug nanocrystals (NCs) on their cellular internalization efficiency, uptake mechanisms, biodistributions as well as in vitro and in vivo antitumor efficiencies. Both confocal imaging and flow cytometry show that shorter NCs with AR = 1.3 have a much faster cellular uptake rate and a much higher anticancer efficacy than longer NCs. All NCs with different ARs were found to enter the cells via an energy-dependent clathrin-mediated pathway. In vivo experiments indicate that NCs with higher ARs have a shorter half-life and are more easily captured by the liver, while the corresponding tumor uptake decreased. We also observed that NCs with the smallest AR have the highest therapeutic efficacy with appreciably less weight loss. These results would assist in the future design of drug NCs and may lead to the development of new drug nanostructures for biomedical applications.

Graphical abstract: The aspect ratio effect of drug nanocrystals on cellular internalization efficiency, uptake mechanisms, and in vitro and in vivo anticancer efficiencies

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Supplementary files

Article information


Submitted
14 Nov 2014
Accepted
17 Jan 2015
First published
19 Jan 2015

Nanoscale, 2015,7, 3588-3593
Article type
Paper
Author version available

The aspect ratio effect of drug nanocrystals on cellular internalization efficiency, uptake mechanisms, and in vitro and in vivo anticancer efficiencies

B. Tian, X. Zhang, C. Yu, M. Zhou and X. Zhang, Nanoscale, 2015, 7, 3588
DOI: 10.1039/C4NR06743F

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