Encapsulation of biophenolic phytochemical EGCG within lipid nanoparticles enhances its stability and cytotoxicity against cancer. (June 2016)

• Record Type: Journal Article
• Authors: Radhakrishnan, Rasika; Kulhari, Hitesh; Pooja, Deep; Gudem, Sagarika; Bhargava, Suresh; Shukla, Ravi; Sistla, Ramakrishna
• Is Part Of: Chemistry and physics of lipids. Volume 198(2016)
• Page Start: 51
• Page End: 60
• Publication Date: 2016-06
• Subjects: Epigallocatechin gallate -- Solid lipid nanoparticles -- Encapsulation -- Stability -- Cytotoxicity; Lipids -- Periodicals; Lipids -- Periodicals; Lipides -- Périodiques; Lipids; Periodicals; Electronic journals; 547.77
• DOI: 10.1016/j.chemphyslip.2016.05.006
• Languages: English
• ISSNs: 0009-3084

Abstract

Graphical abstract: Highlights: Stability of EGCG in different pH conditions was evaluated. Solid lipid nanoparticles were loaded with EGCG and optimized for particle size and surface charge. Physical characterization of the EGCG-loaded nanoparticle was carried out. EGCG-SLN showed increased cytotoxicity to cancer cells as compared to pure EGCG. Abstract: Epigallocatechin gallate (EGCG), a green tea polyphenolic catechin, has been known to possess a variety of beneficial biological activities. The in-vitro anti-cancer activity of EGCG is well documented. However, the use of EGCG in modern therapeutics is limited due to its poor bioavailability and limited stability at physiological pH. In this study, we have investigated the stability profiles of EGCG in aqueous solutions using UV–vis spectroscopy. Stability results showed very low stability profile of EGCG at physiological pH with rapid degradation under alkaline conditions. Therefore, we have encapsulated EGCG in solid lipid nanoparticles to increase its stability and evaluated for anticancer activity. The lipid core of nanoparticles not only provides an additional structural reinforcement to the nanoparticle assembly, but also makes it biologically compatible, thereby enabling a stealth vehicle for efficient drug delivery. EGCG loaded nanoparticles (EGCG-SLN) were characterized using dynamic light scattering, Fourier transform infrared spectroscopy and differential scanning calorimetry. EGCG and EGCG-SLN were evaluated for their anticancer activities by cellular proliferation. The cytotoxicity of EGCG-SLN was found to be 8.1 times higher against MDA-MB 231 human breast cancer cells and 3.8 times higher against DU-145 human prostate cancer cells than that of the pure EGCG.