The Development of Hyaluronan/Fucoidan-Based Nanoparticles as Macrophages Targeting an Epigallocatechin-3-Gallate Delivery System

Abstract

The aim of this study was to develop a macrophage-targeted nanoparticle composed of hyaluronan/fucoidan complexes with polyethylene glycol-gelatin to encapsulate and deliver epigallocatechin-3-gallate (EGCG), a compound that can regulate macrophage activation and pro-inflammatory mediator production. We show that our nanoparticles can successfully bond to macrophages and deliver more EGCG than an EGCG solution treatment, confirming the anti-inflammatory effects of these nanoparticles in lipopolysaccharide-stimulated macrophages. The prepared nanoparticles were established with a small mean particle size (217.00 ± 14.00 nm), an acceptable polydispersity index (0.28 ± 0.07), an acceptable zeta potential value (−33.60 ± 1.30 mV), and a high EGCG loading efficiency (52.08% ± 5.37%). The targeting abilities of CD44 binding were increased as the hyaluronan concentration increased and decreased by adding a competitor CD44 antibody. Moreover, we found that fucoidan treatment significantly reduced macrophage migration after lipopolysaccharide treatment in a dose-responsive manner. In summary, we successfully created macrophage-targeted nanoparticles for effective targeted delivery of EGCG, which should aid in the development of future anti-inflammatory drugs against macrophage-related diseases.

The potential of functionalized dressing releasing flavonoids facilitates scar-free healing

“…EGCG can be successfully administered to macrophages via the dual-targeted binding method of CS and HA to macrophages. Immunofluorescence tests revealed that following encapsulation, EGCG concentration in macrophages increased dramatically, and intensity increased in a time-dependent way, improving EGCG’s on-target delivery capabilities ( 137 ).…”

Utility of Thermal Cross-Linking in Stabilizing Hydrogels with Beta-Tricalcium Phosphate and/or Epigallocatechin Gallate for Use in Bone Regeneration Therapy

“…Gelatin, derived from collagen, is a polymer that has been widely studied in the medical field owing to its biocompatibility, biodegradability, low cost, and inability to induce an immune reaction in vivo [ 9 , 10 ]. In addition to the use of gelatin alone, the polymers had been fused with other components, such as epigallocatechin gallate (EGCG) [ 11 ] (an extract of green tea that exhibits anti-inflammatory [ 11 ], antibacterial [ 12 ], and antioxidant [ 13 ] effects), growth factors that control cell proliferation and differentiation [ 14 ], and various calcium phosphates [ 15 ] including β-TCP [ 16 ]. Gelatin for medical use—often obtained from bovine bone and pig skin [ 17 ]—has been shown to carry growth factors and promote cell growth [ 18 ].…”