Abstract

Silica nanoparticles (SiO2 NPs) synthesized by the Stober method were used as drug delivery vehicles. Doxorubicin hydrochloride (DOX·HCl) is a chemo-drug absorbed onto the SiO2 NPs surfaces. The DOX·HCl loading onto and release from the SiO2 NPs was monitored via UV-VIS and fluorescence spectra. Alternatively, the zeta potential was also used to monitor and evaluate the DOX·HCl loading process. The results showed that nearly 98% of DOX·HCl was effectively loaded onto the SiO2 NPs’ surfaces by electrostatic interaction. The pH-dependence of the process wherein DOX·HCl release out of DOX·HCl-SiO2 NPs was investigated as well. For comparison, both the free DOX·HCl molecules and DOX·HCl-SiO2 NPs were used as the labels for cultured cancer cells. Confocal laser scanning microscopy images showed that the DOX·HCl-SiO2 NPs were better delivered to cancer cells which are more acidic than healthy cells. We propose that engineered DOX·HCl-SiO2 systems are good candidates for drug delivery and clinical applications.

Highlights

  • Doxorubicin (DOX) is an anthracycline antibiotic and is one of the most chemotherapeutic antitumor drugs to treat different solid malignant tumors

  • DOX consists of a planar anthraquinone nucleus attached to an amino sugar through a glycosidic bond [1]

  • In order to increase aqueous solubility, the amino group of sugar is protonated by forming DOX hydrochloride (DOX·HCl)

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Summary

Introduction

Doxorubicin (DOX) is an anthracycline antibiotic and is one of the most chemotherapeutic antitumor drugs to treat different solid malignant tumors. SiO2 NPs constituents are mainly the siloxane groups that can be broken down via hydrolysis to the orthosilicic acid in the human body after the drug delivery process These products are biocompatible and are excreted well by the urinary system [11,12]. Due to the silanols groups (Si-OH) on the pores and surfaces of SiO2 NPs, which confer a very negative zeta potential, the positively charged drugs can be absorbed onto SiO2 NPs pores and surfaces by the strong electrostatic interaction [13] Knowing this mechanism, one can control the drug-releasing process at the targets [14]. Confocal laser scanning microscopy (LCSM) images showed that the DOX·HCl-SiO2 NPs were efficiently delivered to cancer cells These results show that the DOX·HCl-SiO2 NPs system is an effective method of drug delivery and has great potential for clinical applications

Materials
Cell Culture and Cellular Uptake Assay
Synthesis of SiO2 NPs
Doxorubicin Loading onto the SiO2 NPs Surface
Characterization
Findings
Conclusions

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