Hyaluronic acid - dihydroartemisinin conjugate: Synthesis, characterization and in vitro evaluation in lung cancer cells.

Authors:
Robin Kumar
Robin Kumar
National Institute of Immunology
New Delhi | India
Mamta Singh
Mamta Singh
All India Institute of Medical Sciences
New Delhi | India
Jairam Meena
Jairam Meena
Neurotherapeutics Lab
Durairaj Thiyagarajan
Durairaj Thiyagarajan
Indian Institute of Technology Guwahati
Mr. Ankit Saneja, M.S. (Pharm.), Ph.D.
Mr. Ankit Saneja, M.S. (Pharm.), Ph.D.
CSIR-Indian Institute of Integrative Medicine
Pharmaceutics
Jammu, Jammu & Kashmir | India
Amulya K Panda
Amulya K Panda
National Institute of Immunology
New Delhi | India

Int J Biol Macromol 2019 Jul 17;133:495-502. Epub 2019 Apr 17.

Product Development Cell, National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi 110067, India. Electronic address:

In recent years, a great deal of attention has been given towards re-purposing and re-innovating the potential drugs. In this regard, dihydroartemisinin (DHA) has been reported to demonstrate anti-proliferative effects on various cancerous cells viz. breast, liver and lung. However, it is associated with some limitations, such as low bioavailability which is hampered by its poor aqueous solubility and its rapid metabolism in systemic circulation. Therefore, in order to overcome these limitations, we synthesized a novel hyaluronic acid-dihydroartemisinin conjugate in which the hydroxyl group of DHA was covalently linked to carboxylic group of hyaluronic acid (HA). The conjugate was successfully characterized using H NMR, Fourier transform infrared spectroscopy (FT-IR) and gel permeation chromatography (GPC). The synthesized conjugate self-assembled into nanoparticles in aqueous solution. The developed nanoparticles were characterized for their average size, zeta potential, Transmission Electron Microscopy (TEM), X-ray Powder Diffraction (XRD) and loading efficiency. The nanoparticles were cytotoxic to lung cancer (A549) cell line which was determined using CCK-8 cell viability assay. This was further supported by Annexin-V-FITC-Propidium iodide apoptosis assay, reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP) loss. Conclusively, present findings demonstrate hyaluronic acid conjugates can be used to improve the therapeutic outcomes of anticancer drugs.

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http://dx.doi.org/10.1016/j.ijbiomac.2019.04.124DOI Listing
July 2019
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