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Nanoparticles' Surface Charge Influences Tumor Penetration and Therapeutic Efficacy

May 19, 2016

Physiochemical properties of cancer nanoparticle medicines such as size, shape and surface properties decide their in vivo fate and therapeutic efficacy. However, the correlation between nanoparticles’ surface charge and its tumor penetration capability and its impact on therapeutic effect are still in mystery. A recent study jointly conducted by research teams led by Prof. WANG Jun and Prof. WANG Yucai at University of Science & Technology of China of Chinese Academy of Sciences revealed that positively charged PEGylated polymeric nanoparticles (NPs) possess improved penetration ability over neutral or negatively charged NPs in the interstitial tumor space. This study was published online in Nano Today. 

To find out how the surface charge influences the tumor penetration, researchers prepared a series of NPs from PEG-b-PLA, and tuned their surface charges with different lipid components. The NPs with different charges were categorized into three groups: positive, neutral and negative. The researchers assessed the NPs’ cellular uptake, pharmacokinetics and antitumor efficacy in MDA-MB-231orthotopic tumors to evaluate the NPs’ antitumor activity. Also, they tested these NPs’ penetration efficiency in in vitro three dimensional multicellular spheroids (MCSs) and transwell models. 

Results indicated that cationic PEGylated nanoparticles exhibit much better performance in inhibiting tumor growth in five different tumor models than the anionic and neutral counterparts. Docetaxel-loaded cationic nanoparticles significantly suppressed tumor growth with an inhibition ratio of 90%, compared with the 60% achieved by their anionic or neutral counterparts. The study also revealed that superior treatment efficacy of cationic PEGylated’ nanoparticles is based on their better tumor penetration and 2.5-fold higher cellular uptake. 

This research provides insights into understanding the physiochemical properties’ of nanomedicine role in its in-vivo application. 

The research was supported by the National Basic Research Program of China (973 Programs, 2012CB932500, 2015CB932100 and 2013CB933900), the National Natural Science Foundation of China (51125012, 51390482) and NIH (HL109442 and AI096305). 

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