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Issue 10, 2018
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A pH-sensitive guar gum-grafted-lysine-β-cyclodextrin drug carrier for the controlled release of 5-flourouracil into cancer cells

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Abstract

The physiological environment is a crucial factor in biomedical systems, which can be regulated with relative ease both in vitro and in vivo. Control of pH has emerged as a powerful strategy in cancer therapy because pH has a profound effect on the interaction of a polymeric-based drug delivery system with tumor cells. In this regard, the enhancement of pH response capability was demonstrated with a 5-flourouracil (5-FU)-loaded guar gum (GG)-grafted-lysine-β-cyclodextrin (L-β-CD) drug carrier. The size, charge, morphology, and encapsulation efficiency of the 5-FU-loaded polymeric carrier were characterized for the control and sustained release of the drug. In a specific cancer pH environment, 5-FU-loaded GG-g-L-β-CD could rapidly swallow, disassemble, and release 5-FU by accepting or losing electrons. In vitro observations indicate that GG-g-L-β-CD dramatically releases 5-FU in an acidic environment rather than in a basic environment. In vitro antitumor activity tests showed that 5-FU-loaded GG-g-L-β-CD had a higher cytotoxicity against KB cells, with an IC50 value of 1.38 μg ml−1. The reactive oxygen species (ROS) generated by 5-FU in the KB cells showed efficient suppression of tumour cell growth. The Hoechst assay revealed the active nature of 5-FU in the cell nucleus of the KB cells. The potential mitochondrial damage by apoptosis in KB cells greatly increased cell death. Therefore, due to its active nature, the pH-sensitive 5-FU-loaded GG-g-L-β-CD carrier is a potential drug delivery system for safe and effective cancer therapy, and it can be useful for inhibiting tumour cell growth.

Graphical abstract: A pH-sensitive guar gum-grafted-lysine-β-cyclodextrin drug carrier for the controlled release of 5-flourouracil into cancer cells

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Supplementary files

Article information


Submitted
23 Sep 2017
Accepted
09 Feb 2018
First published
09 Feb 2018

J. Mater. Chem. B, 2018,6, 1519-1530
Article type
Paper

A pH-sensitive guar gum-grafted-lysine-β-cyclodextrin drug carrier for the controlled release of 5-flourouracil into cancer cells

R. A. Praphakar, M. Jeyaraj, S. Mehnath, A. Higuchi, D. Ponnamma, K. K. Sadasivuni and M. Rajan, J. Mater. Chem. B, 2018, 6, 1519
DOI: 10.1039/C7TB02551C

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