Fabrication of chitosan-coated epigallocatechin-3-gallate (EGCG)-hordein nanoparticles and their transcellular permeability in Caco-2/HT29 cocultures

• Published in: International journal of biological macromolecules Vol. 196; pp. 144 - 150
• Main Authors: Song, Hongdong, He, Aijing, Guan, Xiao, Chen, Zhengyu, Bao, Yize, Huang, Kai
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 31.01.2022
• Subjects: Biological Transport; Caco-2 Cells; Catechin - analogs & derivatives; Catechin - chemistry; Cell Line; Cells, Cultured; Chitosan - chemistry; Drug Carriers - chemistry; Epigallocatechin-3-gallate; Glutens - chemistry; Humans; Nanoparticles - chemistry; Particle Size; Permeability; Spectrum Analysis; Transcellular transport; Uptake mechanism; Transcellular transport; Epigallocatechin-3-gallate; Uptake mechanism
• ISSN: 0141-8130; 1879-0003
• DOI: 10.1016/j.ijbiomac.2021.12.024

Epigallocatechin-3-gallate (EGCG) has gained appreciable attention because of its health benefits. However, the poor permeability across the intestine limits its use. In this study, we have fabricated chitosan-coated EGCG-hordein nanoparticles (Cs-EHNs), with the aim to enhance the intestinal permeability of EGCG. Cs-EHNs were fabricated by layer-by-layer electrostatic stacking method, and its uptake and transcellular permeability were studied in the Caco-2/HT29 co-culture model. The constructed Cs-EHNs had the average diameter of 296 nm, polymer dispersity index (PDI) of 0.30, zeta potential of 59.6 mV, and showed a spherical morphology. Encapsulation efficiency of EGCG was 87.3%. The transcellular permeability experiments indicated that the apparent permeability coefficient (Papp) of Cs-EHNs was higher than that of free EGCG. Furthermore, the cellular uptake of Cs-EHNs was studied by specific endocytosis inhibitors, and results showed that the uptake mechanisms of Cs-EHNs were through caveolae-mediated endocytosis and macropinocytosis. This study demonstrated that encapsulation of EGCG using chitosan-coated hordein nanoparticles could be a promising approach to improve the absorption of EGCG. [Display omitted] •Chitosan-coated EGCG-hordein nanoparticles (Cs-EHNs) were fabricated by layer-by-layer electrostatic stacking method.•Uptake and transcellular permeability of Cs-EHNs were studied in the Caco-2/HT29 co-culture model.•Cs-EHNs could significantly increase the transcellular permeability of EGCG than free EGCG.•Uptake mechanisms of Cs-EHNs were through caveolae-mediated endocytosis and macropinocytosis.