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Phenylboronic Acid-Mediated Tumor Targeting of Chitosan Nanoparticles

Phenylboronic Acid-Mediated Tumor Targeting of Chitosan Nanoparticles

Xin Wang, Huang Tang, Chongzhi Wang, Jialiang Zhang, Wei Wu, Xiqun Jiang

Theranostics. 2016 Jun 15;6(9):1378-92.

PMID: 27375786

Abstract:

The phenylboronic acid-conjugated chitosan nanoparticles were prepared by particle surface modification. The size, zeta potential and morphology of the nanoparticles were characterized by dynamic light scattering, zeta potential measurement and transmission electron microscopy. The cellular uptake, tumor penetration, biodistribution and antitumor activity of the nanoparticles were evaluated by using monolayer cell model, 3-D multicellular spheroid model and H22 tumor-bearing mice. The incorporation of phenylboronic acid group into chitosan nanoparticles impart a surface charge-reversible characteristic to the nanoparticles. In vitro evaluation using 2-D and 3-D cell models showed that phenylboronic acid-decorated nanoparticles were more easily internalized by tumor cells compared to non-decorated chitosan nanoparticles, and could deliver more drug into tumor cells due to the active targeting effect of boronic acid group. Furthermore, the phenylboronic acid-decorated nanoparticles displayed a deeper penetration and persistent accumulation in the multicellular spheroids, resulting in better inhibition growth to multicellular spheroids than non-decorated nanoparticles. Tumor penetration, drug distribution and near infrared fluorescence imaging revealed that phenylboronic acid-decorated nanoparticles could penetrate deeper and accumulate more in tumor area than non-decorated ones. In vivo antitumor examination demonstrated that the phenylboronic acid-decorated nanoparticles have superior efficacy in restricting tumor growth and prolonging the survival time of tumor-bearing mice than free drug and drug-loaded chitosan nanoparticles.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP849062233	3-Bromo-5-methyl-2-(3′-methoxybenzyloxy)phenylboronic acid	849062-23-3	Price
LS793678	(3-acetamido-5-carboxy)phenylboronic acid		Price
LS793961	3-(trans-4-Hydroxycyclohexylcarbamoyl)phenylboronic acid		Price

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