Abstract
In this study, we synthesized dendrimer-functionalized laponite (LAP) nanodisks for loading and delivery of anticancer drug doxorubicin (DOX). Firstly, LAP was modified with silane coupling agents and succinic anhydride to render abundant carboxyl groups on the surface of LAP. Then, poly(amidoamine) (PAMAM) dendrimer of generation 2 (G2) were conjugated to form LM-G2 nanodisks. Anticancer drug DOX was then loaded on the LM-G2 with an impressively high drug loading efficiency of 98.4% and could be released in a pH-sensitive and sustained manner. Moreover, cell viability assay results indicate that LM-G2/DOX complexes could more effectively inhibit the proliferation of KB cells (a human epithelial carcinoma cell line) than free DOX at the same drug concentration. Flow cytometry analysis and confocal laser scanning microscope demonstrated that LM-G2/DOX could be uptaken by KB cells more effectively than free DOX. Considering the exceptional high drug loading efficiency and the abundant dendrimer amine groups on the surface that can be further modified, the developed LM-G2 nanodisks may hold a great promise to be used as a novel platform for anticancer drug delivery.
Highlights
Cancer is one of the most significant threats to human health and will cause about 15 million deaths in 2020 [1]
In order to demonstrate the modification of APMES and generation 2 (G2) on the LAP nanodisks, LM-G2 nanodisks were characterized by thermogravimetric analysis (TGA) (Figure 2)
°C, LM-G2 displayed about 5.13% weight loss, which may be ascribed to the amount of G2 dendrimer modified onto LAP nanodisks (This means that 51.3 μg of G2 dendrimers were conjugated onto each milligram of LAP)
Summary
Cancer is one of the most significant threats to human health and will cause about 15 million deaths in 2020 [1]. After modified with folic acid or lactobionic acid as targeting agents via the linkage of silane coupling agents, LAP-based drug delivery systems could deliver anticancer drugs to tumor cells and enhance the inhibition effect of cancer cells [15,16]. This kind of surface modification may cause a decrease in drug loading efficiency. To the best of our knowledge, this is the first report related to the modification of dendrimers onto LAP nanodisks for the efficient delivery of anticancer drugs
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