title: Encapsulation of biophenolic phytochemical EGCG within lipid nanoparticles enhances its stability and cytotoxicity against cancer.
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.
authors.affiliation: 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 Industrial Chemistry, School of Science, RMIT University, Melbourne, Australia.
authors.forename: Rasika
authors.initials: R
authors.lastname: Radhakrishnan
authors.affiliation: 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.
authors.forename: Hitesh
authors.initials: H
authors.lastname: Kulhari
authors.affiliation: Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Deep
authors.initials: D
authors.lastname: Pooja
authors.affiliation: Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Sagarika
authors.initials: S
authors.lastname: Gudem
authors.affiliation: IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical Technology, Hyderabad, India; Centre for Advanced Materials and Industrial Chemistry, School of Science, RMIT University, Melbourne, Australia.
authors.forename: Suresh
authors.initials: S
authors.lastname: Bhargava
authors.affiliation: IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical Technology, Hyderabad, India; Centre for Advanced Materials and Industrial Chemistry, School of Science, RMIT University, Melbourne, Australia.
authors.forename: Ravi
authors.initials: R
authors.lastname: Shukla
authors.affiliation: 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. Electronic address: sistla@iict.res.in.
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Sistla
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D002214:Capsules; D002392:Catechin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004355:Drug Stability; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002214:Capsules; D004337:Drug Carriers; D008055:Lipids; D002392:Catechin; C045651:epigallocatechin gallate
keywords: Cytotoxicity; Encapsulation; Epigallocatechin gallate; Solid lipid nanoparticles; Stability