Abstract

The aim of this study was to prepare and characterize an innovative hepatocellular carcinoma-targeted therapeutic drug delivery system based on folate-PEG-mesoporous silica nanoparticles (FA-PEG-MSNs) loaded with paclitaxel (PTX). In vitro cell experiments and an in vivo antitumor efficacy study demonstrated that FA-PEG-MSNs-PTX produced significantly higher tumor inhibition compared with pure PTX and mesoporous silica nanoparticles loaded with paclitaxel (MSNs-PTX). The biodistribution investigation of PTX in nude mice revealed that the FA-PEG-MSNs-PTX could accumulate in tumors. Folic acid functionalized MSNs resulted in a good targeting effect, confirming that FA-PEG-MSNs-PTX is a promising tumor-targeted drug delivery system for liver cancer chemotherapy.

Highlights

  • In recent years, the incidence of liver cancer has been rapidly increasing

  • NH2-PEG-COOH, N-hydroxysuccinimide (NHS), dicyclohexyl carbodiimide (DCC), 1-ethyl-3[3-dimethylaminopropyl] carbodiimide hydrochloride (EDC), cetyltrimethyl ammonium bromide (CTAB), tetraethyl orthosilicate (TEOS), sodium dodecyl sulfate (SDS), 3-aminopropyltriethoxysilane (APTES), pyridine butylparaben, dimethyl sulfoxide (DMSO), ammonia, ethanol, methanol, and hydroxypropyl methylcellulose (HPMC) were all obtained from Sinopharm Chemical Reagent Company, Ltd. (Shanghai, China) while thiazolyl blue tetrazolium bromide (MTT), Annexin V-FITC Apoptosis Detection Kits, and trypsin were supplied by Nanjing Jiancheng Bioengineering Institute (Nanjing, China)

  • Modification of MSNs with FA-PEG was confirmed by Fourier transform infrared (FTIR) (Figure 3(b))

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Summary

Introduction

The incidence of liver cancer has been rapidly increasing. 782,000 liver cancer cases are diagnosed and 745,000 deaths are reported annually [1]. Because of low survival rates and poor prognosis, it has become the second most common cause of cancer death worldwide [2]. China has the highest number of cases of hepatocarcinoma [3]. Conventional anticancer drugs can affect healthy tissues as well as tumors. Normal cells are destroyed, which results in undesirable side effects such as tissue damage, inflammation, or lesions [6,7,8]. Multidrug resistance of cancer cells to anticancer drugs is an acute problem in the treatment of cancer

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