Facile Synthesis and Characterization of Quercetin-Loaded Alginate Nanoparticles for Enhanced In Vitro Anticancer Effect

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ORIGINAL PAPER

Facile Synthesis and Characterization of Quercetin-Loaded Alginate Nanoparticles for Enhanced In Vitro Anticancer Effect Against Human Leukemic Cancer U937 Cells Sureshkumar Selvaraj1 • Suguna Shanmugasundaram1,2 • Murugan Maruthamuthu1 • Baskar Venkidasamy3 Sambandam Shanmugasundaram4



Received: 4 May 2020 / Accepted: 8 October 2020  Springer Science+Business Media, LLC, part of Springer Nature 2020

Abstract Nanoparticles synthesized from biopolymers have received attention for their use as biological carriers in the delivery of hydrophobic drugs. Alginate, a marine biopolymer, is utilized to synthesize nanoparticles as a nanocarrier to overcome the limitations of quercetin solubility and its bioavailability. The present study aims at the synthesis of alginate nanoparticles (ALG NPs) by a simple approach for the delivery of a bioactive compound, quercetin. Quercetin entrapped alginate nanoparticles (QR-ALG NPs) with a size of 180 nm and negative zeta potential of - 21.4 mV were synthesized following a cold precipitation method. QR-ALG NPs were analyzed by UV, Fluorescence spectroscopy, AFM, SEM, XRD, and FTIR. The formulated QR-ALG NPs achieved a drug entrapment efficiency of 68% along with a shelf life of 35 days at room temperature. In vitro drug release assay showed a sustainable quercetin release up to 6 days. DPPH assay showed that QR-ALG NPs retained its antioxidant activity. MTT results demonstrated that QR-ALG NPs enhanced anticancer efficacy on the U937 cell line. This novel method to synthesize ALG NP is simple, efficient, and less laborious, could be a promising application for encapsulating drugs in nanomedicine.

& Sureshkumar Selvaraj [email protected] 1

Department of Microbial Technology, School of Biological Sciences, Madurai Kamaraj University, Madurai 625021, Tamilnadu, India

2

Formerly, Research and Development, Reliance Industries Ltd, Jamnagar 361140, India

3

Department of Biotechnology, Bharathiar University, Coimbatore 641046, Tamilnadu, India

4

Department of Biotechnology, Sri Shakthi Institute of Engineering and Technology, Coimbatore 641062, Tamilnadu, India

123

S. Selvaraj et al.

Graphic abstract

Keywords Quercetin  Alginate  Drug delivery  U-937  Antioxidant  Anticancer  Nanoparticles

Introduction Alginates (ALG) are the natural polymers obtained from brown algae. The unique properties of alginates, such as biocompatibility, mucoadhesive nature, non-immunogenicity, and low production cost, make it a polymer of choice for various applications. Alginate is a linear polysaccharide consisting of 1, 4 linked b-D-mannuronic acid (M) and a-L-guluronic acid (G) residues and forms hydrogels [1]. The hydroxyl (–OH) and carboxyl (–COOH) functional group of alginate make it stable in acidic environments and exhibits controlled drug delivery when used as a nanocarrier of drugs [2]. The bioadhesive nature of alginate favors intestinal adsorption, and therefore, oral administration of alginate entrapped drugs with