In vitro study on anti-inflammatory effects of epigallocatechin-3-gallate-loaded nano- and microscale particles

Abstract

Purpose

This study aimed to develop an anti-inflammation system consisting of epigallo-catechin-3-gallate (EGCG) encapsulated in poly(lactide-co-glycolic acid) (PLGA) particles to promote wound healing.

Methods

Nano- and microscale PLGA particles were fabricated using a water/oil/water emulsion solvent evaporation method. The optimal particle size was determined based on drug delivery efficiency and biocompatibility. The particles were loaded with EGCG. The anti-inflammatory effects of the particles were evaluated in an in vitro cell-based inflammation model.

Results

Nano- and microscale PLGA particles were produced. The microscale particles showed better biocompatibility than the nanoscale particles. In addition, the microscale particles released ~60% of the loaded drug, while the nanoscale particles released ~50%, within 48 hours. Thus, microscale particles were selected as the carriers. The optimal EGCG working concentration was determined based on the effects on cell viability and inflammation. A high EGCG dose (100 μM) resulted in poor cell viability; therefore, a lower dose (≤50 μM) was used. Moreover, 50 μM EGCG had a greater anti-inflammatory effect than 10 μM concentration on lipopolysaccharide-induced inflammation. Therefore, 50 μM EGCG was selected as the working dose. EGCG-loaded microparticles inhibited inflammation in human dermal fibroblasts. Interestingly, the inhibitory effects persisted after replacement of the drug-loaded particle suspension solution with fresh medium.

Conclusion

The EGCG-loaded microscale particles are biocompatible and exert a sustained anti-inflammatory effect.