Folate-targeted nanostructured lipid carriers for enhanced oral delivery of epigallocatechin-3-gallate

• Published in: Food chemistry Vol. 237; pp. 803 - 810
• Main Authors: Granja, Andreia, Vieira, Alexandre C., Chaves, Luíse L., Nunes, Cláudia, Neves, Ana Rute, Pinheiro, Marina, Reis, Salette
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.12.2017
• Subjects: Catechin - analogs & derivatives; Catechin - chemistry; Drug Carriers; Folic Acid; Food enrichment; Humans; In vitro release; Lipids; Nanostructures - chemistry; Nutraceutic; Oral bioavailability; Polyphenol; Supplement; Supplement; In vitro release; Polyphenol; Oral bioavailability; Food enrichment; Nutraceutic
• ISSN: 0308-8146; 1873-7072
• DOI: 10.1016/j.foodchem.2017.06.019

•EGCG was encapsulated into NLC to improve its intestinal permeability and stability.•Parameters such as size, EE and LC were optimized using a Box-Behnken design.•An in vitro release study in simulated gastric and intestinal fluids was performed.•NLC formulations revealed suitable properties for the oral delivery of EGCG.•EGCG-loaded NLC have potential for food enrichment and therapeutic supplementation. The well-known pleiotropic health benefits of green tea are mainly attributed to epigallocatechin-3-gallate (EGCG), a polyphenolic compound from the group of catechins. EGCG’s poor stability and intestinal permeability, however, can strongly impair its biological activities. In this work, EGCG-loaded nanostructured lipid carriers (NLC) functionalized with folic acid were optimized through a Box-Behnken design intended to provide an enhanced oral absorption and increased bioavailability of EGCG. Size, zeta potential and encapsulation efficiency (EE) of the produced spherical nanoparticles were evaluated. NLC were further characterized by Differential Scanning Calorimetry (DSC). An in vitro release study in simulated gastric and intestinal fluids was conducted and the storage stability of the nanoparticles was evaluated over a period of 8weeks. The overall results demonstrated the suitability of the developed formulation for the oral delivery of EGCG and its potential for applications in food industry.