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Article

Increased Cytotoxic Efficacy of Protocatechuic Acid in A549 Human Lung Cancer Delivered via Hydrophobically Modified-Chitosan Nanoparticles As an Anticancer Modality

1
Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Selangor 43400, Malaysia
2
Department of Human Anatomy, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Selangor 43400, Malaysia
3
UPM-MAKNA Cancer Research Laboratory, Institute of Biosciences, Universiti Putra Malaysia, Selangor 43400, Malaysia
*
Author to whom correspondence should be addressed.
Polymers 2020, 12(9), 1951; https://doi.org/10.3390/polym12091951
Received: 10 July 2020 / Revised: 31 July 2020 / Accepted: 31 July 2020 / Published: 28 August 2020
(This article belongs to the Special Issue Functional Chitosan-Based Composites)
The growing incidence of global lung cancer cases against successful treatment modalities has increased the demand for the development of innovative strategies to complement conventional chemotherapy, radiation, and surgery. The substitution of chemotherapeutics by naturally occurring phenolic compounds has been touted as a promising research endeavor, as they sideline the side effects of current chemotherapy drugs. However, the therapeutic efficacy of these compounds is conventionally lower than that of chemotherapeutic agents due to their lower solubility and consequently poor intracellular uptake. Therefore, we report herein a hydrophobically modified chitosan nanoparticle (pCNP) system for the encapsulation of protocatechuic acid (PCA), a naturally occurring but poorly soluble phenolic compound, for increased efficacy and improved intracellular uptake in A549 lung cancer cells. The pCNP system was modified by the inclusion of a palmitoyl group and physico-chemically characterized to assess its particle size, Polydispersity Index (PDI) value, amine group quantification, functional group profiling, and morphological properties. The inclusion of hydrophobic palmitoyl in pCNP-PCA was found to increase the encapsulation of PCA by 54.5% compared to unmodified CNP-PCA samples whilst it only conferred a 23.4% larger particle size. The single-spherical like particles with uniformed dispersity pCNP-PCA exhibited IR bands, suggesting the successful incorporation of PCA within its core, and a hydrophobic layer was elucidated via electron micrographs. The cytotoxic efficacy was then assessed by using an MTT cytotoxicity assay towards A549 human lung cancer cell line and was compared with traditional chitosan nanoparticle system. Fascinatingly, a controlled release delivery and enhanced therapeutic efficacy were observed in pCNP-PCA compared to CNP, which is ascribed to lower IC50 values in the 72-h treatment in the pCNP system. Using the hydrophobic system, efficacy of PCA was significantly increased in 24-, 48-, and 72-h treatments compared to a single administration of the compound, and via the unmodified CNP system. Findings arising from this study exhibit the potential of using such modified nanoparticulate systems in increasing the efficacy of natural phenolic compounds by augmenting their delivery potential for better anti-cancer responses. View Full-Text
Keywords: hydrophobically modified-chitosan nanoparticle; protocatechuic acid; nanobiotechnology hydrophobically modified-chitosan nanoparticle; protocatechuic acid; nanobiotechnology
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MDPI and ACS Style

Yee Kuen, C.; Galen, T.; Fakurazi, S.; Othman, S.S.; Masarudin, M.J. Increased Cytotoxic Efficacy of Protocatechuic Acid in A549 Human Lung Cancer Delivered via Hydrophobically Modified-Chitosan Nanoparticles As an Anticancer Modality. Polymers 2020, 12, 1951. https://doi.org/10.3390/polym12091951

AMA Style

Yee Kuen C, Galen T, Fakurazi S, Othman SS, Masarudin MJ. Increased Cytotoxic Efficacy of Protocatechuic Acid in A549 Human Lung Cancer Delivered via Hydrophobically Modified-Chitosan Nanoparticles As an Anticancer Modality. Polymers. 2020; 12(9):1951. https://doi.org/10.3390/polym12091951

Chicago/Turabian Style

Yee Kuen, Cha, Tieo Galen, Sharida Fakurazi, Siti S. Othman, and Mas J. Masarudin 2020. "Increased Cytotoxic Efficacy of Protocatechuic Acid in A549 Human Lung Cancer Delivered via Hydrophobically Modified-Chitosan Nanoparticles As an Anticancer Modality" Polymers 12, no. 9: 1951. https://doi.org/10.3390/polym12091951

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