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Chitosan-Based Nanomaterials for Drug Delivery
Open AccessArticle

Galactosylated Chitosan-Functionalized Mesoporous Silica Nanoparticle Loading by Calcium Leucovorin for Colon Cancer Cell-Targeted Drug Delivery

1
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China
2
Department of Pharmaceutics, School of Pharmacy, Zhengzhou University, 100 Science Avenue, Zhengzhou 450001, China
*
Author to whom correspondence should be addressed.
Academic Editor: Jyh-Ping Chen
Molecules 2018, 23(12), 3082; https://doi.org/10.3390/molecules23123082
Received: 31 October 2018 / Revised: 20 November 2018 / Accepted: 23 November 2018 / Published: 26 November 2018
(This article belongs to the Special Issue Chitosan-Based Nanomaterials for Biomedical Applications)
Targeted drug delivery to colon cancer cells can significantly improve the efficiency of treatment. We firstly synthesized carboxyl-modified mesoporous silica nanoparticles (MSN–COOH) via two-step synthesis, and then developed calcium leucovorin (LV)-loaded carboxyl-modified mesoporous silica nanoparticles based on galactosylated chitosan (GC), which are galectin receptor-mediated materials for colon-specific drug delivery systems. Both unmodified and functionalized nanoparticles were characterized by scanning electron microscopy (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), Fourier transform infrared (FT-IR), nitrogen sorption, and dynamic light scattering (DLS). Drug release properties and drug loading capacity were determined by ultraviolet spectrophotometry (UV). [email protected]–COOH/GC had a high LV loading and a drug loading of 18.07%. In vitro, its release, mainly by diffusion, was sustained release. Cell experiments showed that in SW620 cells with the galectin receptor, the [email protected]–COOH/GC metabolized into methyl tetrahydrofolic acid (MTHF) and 5-fluorouracil (5-FU)@MSN–NH2/GC metabolized into FdUMP in vivo. MTHF and 5-fluoro-2′-deoxyuridine 5′-monophosphate (FdUMP) had combined inhibition and significantly downregulated the expression of thymidylate synthase (TS). Fluorescence microscopy and flow cytometry experiments show that MSN–COOH/GC has tumor cell targeting, which specifically recognizes and binds to the galectin receptor in tumor cells. The results show that the nano-dosing system based on GC can increase the concentrations of LV and 5-FU tumor cells and enhance their combined effect against colon cancer. View Full-Text
Keywords: calcium leucovorin; MSN–COOH; galactosylated chitosan (GC); [email protected]–COOH/GC; galectin receptor; SW620 cells calcium leucovorin; MSN–COOH; galactosylated chitosan (GC); [email protected]–COOH/GC; galectin receptor; SW620 cells
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MDPI and ACS Style

Liu, W.; Wang, F.; Zhu, Y.; Li, X.; Liu, X.; Pang, J.; Pan, W. Galactosylated Chitosan-Functionalized Mesoporous Silica Nanoparticle Loading by Calcium Leucovorin for Colon Cancer Cell-Targeted Drug Delivery. Molecules 2018, 23, 3082.

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