Abstract
As a part of research project aimed to optimize antioxidant delivery, here we studied the influence of both salts and lipid matrix composition on the interaction of epigallocatechin-3-gallate (EGCG) with bilayer leaflets. Thus, we combined in silico and experimental methods to study the ability of neutral and anionic vesicles to encapsulate EGCG in the presence of Ca2+ and Mg2+ divalent salts. Experimental and in silico results show a very high correlation, thus confirming the efficiency of the developed methodology. In particular, we found out that the presence of calcium ions hinders the insertion of EGCG in the liposome bilayer in both neutral and anionic systems. On the contrary, the presence of MgCl2 improves the insertion degree of EGCG molecules respect to the liposomes without divalent salts. The best and most efficient salt concentration is that corresponding to a 5:1 molar ratio between Mg2+ and EGCG, in both neutral and anionic vesicles. Concerning the lipid matrix composition, the anionic one results in better promotion of the catechin insertion within the bilayer since experimentally we achieved 100% EGCG encapsulation in the lipid carrier in the presence of a 5:1 molar ratio of magnesium. Thus, the combination of this anionic liposomal formulation with magnesium chloride, avoids time-consuming separation steps of unentrapped active principle and appears particularly suitable for EGCG delivery applications.
Highlights
Nanostructures made of amphiphilic natural or synthetic lipids are biocompatible and biodegradable platforms for drug delivery [1,2,3,4,5,6,7,8,9]
We found out that the presence of calcium ions hinders the insertion of EGCG in the liposome bilayer in both neutral and anionic systems
This can be explained considering that calcium ions interact more efficiently with lipids’ phosphate groups compared to EGCG, so the corresponding percentage of catechin encapsulation observed experimentally is very low
Summary
Nanostructures made of amphiphilic natural or synthetic lipids are biocompatible and biodegradable platforms for drug delivery [1,2,3,4,5,6,7,8,9]. Liposomes present some important advantages: for example, they can increase the stability of the encapsulated molecules and improve their pharmacokinetic effect by reducing elimination and enhancing circulation lifetimes. The use of EGCG as a drug or natural additive is compromised by its oxidizability and instability that determine a poor bioavailability within the biological system whatever the administration mode is [18,19,20]. Epigallocatechin-3-gallate (EGCG) is the major constituent in green tea [11]; it presents remarkable bioactivity ranging from anticancer [12,13] to cancer- and in general age-associated pathology prevention effects [14,15] as well as regulation of the immune [16] and endocrine systems [17].
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
