Research Papers:

Vincristine liposomes with smaller particle size have stronger diffusion ability in tumor and improve tumor accumulation of vincristine significantly

Siyu Ma, Mingyuan Li, Nan Liu, Ying Li, Zhiping Li, Yang Yang, Fanglin Yu, Xiaoqin Hu, Cheng Liu and Xingguo Mei _

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Oncotarget. 2017; 8:87276-87291. https://doi.org/10.18632/oncotarget.20162

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Siyu Ma1,2,*, Mingyuan Li1,3,*, Nan Liu1, Ying Li1, Zhiping Li1, Yang Yang1, Fanglin Yu1, Xiaoqin Hu1,2, Cheng Liu1,2 and Xingguo Mei1

1Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, PR China

2Wuhan Institute of Technology, Wuhan, PR China

3China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Sino-French Joint Lab of Food Nutrition/Safety and Medicinal Chemistry, Key Laboratory of Industrial Fermentation Microbiology of Ministry of Education, Tianjin Key Laboratory of Industry Microbiology, College of Biotechnology, Tianjin University of Science and Technology, Tianjin, PR China

*These authors have contributed equally to this work

Correspondence to:

Xingguo Mei, email: [email protected]

Keywords: particle size, diffusion ability, targeting effect, liposome, tumor targeting

Received: February 13, 2017    Accepted: June 20, 2017    Published: August 10, 2017


The passive targeting is the premise of active targeting that could make nanocarrier detained in tumor tissue. The particle size is the most important factor that influences the diffusion and distribution of nanoparticle both in vivo and in vitro. In order to investigate the relationship between particle size and diffusion ability, two kinds of liposome loaded with Vincristine (VCR-Lip) were prepared. The diffusion behavior of VCR-Lip with different particle size and free VCR was compared through diffusion stability study. The diffusion ability from 12-well culture plate to Millipore transwell of each formulation reflected on HepG-2 cytotoxicity results. Different cell placement methods and drug adding positions were used to study the VCR-Lip diffusion behaviors, which influenced the apoptosis of HepG-2 cell. The different cell uptake of Nile red–Lip and free Nile red was compared when changed the adding way of fluorescent fluorescein. To study the penetration ability in HepG-2 tumor spheroids, we constructed 30 nm and 100 nm Cy5.5-Lip to compare with free Cy5.5. Then the anti-tumor effect, tissue distribution of free VCR injection, 30 nm and 100 nm VCR-Lip were further investigated on the HepG-2 tumor bearing nude mice. The results of these study showed that the diffusion ability of free drug and fluorescent fluorescein was remarkable stronger than which encapsulated in liposomes. Moreover, diffusion ability of smaller liposome was stronger than larger one. In this way, 30 nm liposome had not only faster and stronger tumor distribution than 100 nm liposome, but also higher tumor drug accumulation than free drug as well. Our study provided a new thinking to improve the targeting efficiency of nano drug delivery system, no matter passive or active targeting.

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