Issue 11, 2012

Doxorubicin loaded silica nanorattles actively seek tumors with improved anti-tumor effects

Abstract

Silica nanorattles (SNs) have proven to be promising vehicles for drug delivery. In order to further enhance efficacy and minimize adverse effects, active targeted delivery to tumors is necessary. In this work, SNs modified with a tumor specific targeting ligand, folic acid (FA), was used as carrier of doxorubicin (DOX) (DOX–FA-SNs). Drug loading, cytotoxicity and cellular uptake of DOX–FA-SNs in vitro in human cervical carcinoma cells (HeLa cells) were evaluated. DOX–FA-SNs showed a higher cytotoxicity in human cervical carcinoma cells (HeLa cells) than DOX loaded carboxyl (–COOH) and poly(ethylene glycol) (PEG) modified SNs (DOX–COOH-SNs and DOX–PEG-SNs, respectively). However, DOX–FA-SNs showed lower cytotoxicity in folate receptor negative normal mouse fibroblast cells (L929 cells) compared with free DOX. In vivo tumor-targeted fluorescence imaging indicated specific tumor targeting and uptake of FA-SNs in nude mice bearing subcutaneous HeLa cell-derived xenograft tumors. In vivo anti-tumor experiments demonstrated that DOX–FA-SNs (10 mg kg−1 of DOX) significantly regressed the tumor growth and reduced toxicity compared with free DOX. These results have great significance in developing and optimizing SNs as effective intracellular delivery and specific tumor targeting vehicles.

Graphical abstract: Doxorubicin loaded silica nanorattles actively seek tumors with improved anti-tumor effects

Supplementary files

Article information

Article type
Paper
Submitted
25 Dec 2011
Accepted
29 Mar 2012
First published
02 Apr 2012

Nanoscale, 2012,4, 3365-3372

Doxorubicin loaded silica nanorattles actively seek tumors with improved anti-tumor effects

F. Gao, L. Li, T. Liu, N. Hao, H. Liu, L. Tan, H. Li, X. Huang, B. Peng, C. Yan, L. Yang, X. Wu, D. Chen and F. Tang, Nanoscale, 2012, 4, 3365 DOI: 10.1039/C2NR12094A

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