Preparation, Characterization, Optimization, and In vitro Anti-inflammatory Evaluation of Epigallocatechin Gallate (EGCG)-loaded Nanostructured Lipid Carriers.

INTRODUCTION

Sustained joint inflammation and oxidative stress are symptoms of Rheumatoid Arthritis (RA), an autoimmune disorder characterized by chronic inflammation. The present study was designed to prepare Epigallocatechin Gallate (EGCG)-loaded Nanostructured Lipid Carriers (NLCs) for enhanced therapeutic benefits in inflammatory conditions like RA.

METHODS

The NLCs were prepared using lecithin using a modified hot homogenizationultrasonication approach containing an aqueous-to-lipid phase ratio of 3:1 (v/v), where the lipid phase consisted of stearic acid and oleic acid (70:30 ratio), while the aqueous phase contained Tween 80 (2% w/v) and soy lecithin (1% w/v). The effect of drug concentration, lipid-to-drug ratio, or stirring time on particle size, zeta potential, and entrapment efficiency was investigated and optimized using a Box-Behnken design. Solubility profiles and partition coefficients were analyzed by spectrophotometric methods. The antioxidant and anti-inflammatory activity of the optimized EGCG-loaded NLCs was evaluated using an in vitro DPPH, H2O2, and protein denaturation assay as a preliminary screening model.

RESULTS

The optimum EGCG-NLCs showed 82.78% DPPH radical scavenging, 92% H2O2 radical scavenging, and 97.23% inhibition of protein denaturation at high concentration (100 µg/ml).

DISCUSSION: The antioxidant and anti-inflammatory activity of EGCG-NLCs demonstrated their therapeutic acceptability for the topical treatment of inflammatory conditions.

CONCLUSION

In conclusion, EGCG-loaded NLCs demonstrated enhanced stability, bioactivity, and applicability for targeted inflammatory conditions such as rheumatoid arthritis therapy. This nanocarrier holds great promise as a phytochemical vehicle delivery system, which can also be integrated with other sophisticated drug delivery structures and undergo in vivo testing in the future.