Abstract
BackgroundMesoporous silica nanoparticles (MSNs) have several attractive properties as a drug delivery system, such as ordered porous structure, large surface area, controllable particle size as well as interior and exterior dual-functional surfaces. The purpose of this study was to develop novel lactosaminated mesoporous silica nanoparticles (Lac-MSNs) for asialoglycoprotein receptor (ASGPR) targeted anticancer drug delivery.ResultsLac-MSNs with an average diameter of approximately 100 nm were prepared by conjugation of lactose with 3-aminopropyl triethoxysilane modified MSNs. Characterization of Lac-MSNs indicated a huge Brunauer-Emmett-Teller (BET) surface area (1012 m2/g), highly ordered 2D hexagonal symmetry, an unique mesoporous structure with average pore size of 3.7 nm. The confocal microscopy and flow cytometric analysis illustrated Lac-MSNs were effectively endocytosed by ASGPR-positive hepatoma cell lines, HepG2 and SMMC7721. In contrast, non-selective endocytosis of Lac-MSNs was found in ASGPR-negative NIH 3T3 cells. The cellular uptake study showed the internalization process was energy-consuming and predominated by clathrin-mediated pathway. Model drug docetaxel (DTX) was loaded in the mesopores of Lac-MSNs by wetness impregnation method. In vitro cytotoxicity assay showed that DTX transported by Lac-MSNs effectively inhibited the growth of HepG2 and SMMC7721 cells in a time- and concentration- dependent manner.ConclusionsThese results demonstrated that Lac-MSNs could be a promising inorganic carrier system for targeted intracellular anti-cancer drug delivery.
Highlights
Mesoporous silica nanoparticles (MSNs) have several attractive properties as a drug delivery system, such as ordered porous structure, large surface area, controllable particle size as well as interior and exterior dual-functional surfaces
Preparation and characterization of MSNs and Lac-MSNs MSNs were synthesized by the sol–gel method using surfactant as the template
Fluorescein isothiocyanate (FITC) as a fluorescent probe was encapsulated in the Lac-MSNs through co-condensation in order to monitor the interaction between the nanoparticles and the cells [31]
Summary
Mesoporous silica nanoparticles (MSNs) have several attractive properties as a drug delivery system, such as ordered porous structure, large surface area, controllable particle size as well as interior and exterior dual-functional surfaces. The purpose of this study was to develop novel lactosaminated mesoporous silica nanoparticles (Lac-MSNs) for asialoglycoprotein receptor (ASGPR) targeted anticancer drug delivery. Many anticancer drugs have severe toxic side effects due to their unspecific actions on normal cells and tissues [2]. Development of an effective cancer targeting drug delivery system is extremely necessary for improving the drug efficacy to cancer cells, reducing toxic side effects systematically, and prolonging survivals of patients. With recent advances in nanotechnology research, nanocarries have shown great potential to improve the therapeutic efficacy while minimize the side effects, especially for highly toxic anticancer drugs [3,4]. Passive targeting of nanocarriers to these abnormal tumors may be partially achieved with the enhanced permeability and retention (EPR) effect [5,6], leaving the surrounding healthy tissues barely touched. It is expected that the application of nanotechnology would be beneficial to millions of cancer patients with more efficient, safe, and affordable treatment
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