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

Yan Ru Wu,1,* Hong Jin Choi,2,* Yun Gyeong Kang,2 Jeong Koo Kim,1,2 Jung-Woog Shin1–3 1Department of Health Science and Technology, Inje University, Gimhae, Gyeongnam, Republic of Korea; 2Department of Biomedical Engineering, Inje University, Gimhae, Gyeongnam, Republic of Korea; 3Cardiovascular and Metabolic Disease Center, Institute of Aged Life Redesign, UHARC, Inje University, Gimhae, Gyeongnam, Republic of Korea *These authors contributed equally to this work Purpose: This study aimed to develop an anti-inflammation system consisting of epigallocatechin-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. Keywords: wound healing, anti-inflammation, EGCG, microparticles, carriers