Epigallocatechin gallate (EGCG), a green tea polyphenolic catechin, has been known to possess a variety of beneficial biological activities. The anti-cancer activity of EGCG in many cancer cell lines 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-Visible spectroscopy. Stability results showed very low stability profile of EGCG at physiological conditions 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.
Chemistry and physics of lipids. 2016 May 24 [Epub ahead of print]
Rasika Radhakrishnan, Hitesh Kulhari, Deep Pooja, Sagarika Gudem, Suresh Bhargava, Ravi Shukla, Ramakrishna Sistla
Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical technology, Hyderabad, India; IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical technology, Hyderabad, India; Centre for Advanced Materials and Innovative Processing, School of Science, RMIT University, Melbourne, Australia., Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical technology, Hyderabad, India; IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical technology, Hyderabad, India., Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical technology, Hyderabad, India., Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical technology, Hyderabad, India., Centre for Advanced Materials and Innovative Processing, School of Science, RMIT University, Melbourne, Australia., IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical technology, Hyderabad, India; Centre for Advanced Materials and Innovative Processing, School of Science, RMIT University, Melbourne, Australia., Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical technology, Hyderabad, India. Electronic address: .