Preparation and Evaluation of Multitargeted Berberine Microemulsion

Background

Berberine, a phytochemical, possesses remarkable potential for multitargeted drug therapy in microbial infections, wound healing and anti-inflammatory applications. However, its clinical utility in skin and other diseases is constrained due to its high aqueous solubility and inadequate dermal and intestinal absorption, resulting in low absolute bioavailability.

Objectives

The current investigation endeavors to develop a microemulsion loaded with berberine to enhance its solubility and therapeutic effects specifically for skin diseases, while comparing its efficacy with a simple emulsion.

Materials and Methods

In this study, an optimized oil-in- water (o/w) type of emulsion and microemulsion were formulated utilizing berberine isolated from Berberis aristata roots, along with soy lecithin, oleic acid, Tween 80, and ethanol. The microemulsion and emulsion were subjected to characterization employing parameters such as FTIR, particle size, zeta potential, transmittance, viscosity, and stability. The formulations were assessed for their therapeutic effects through in vitro antioxidant, anti-inflammatory, and anti, microbial assays, encompassing six strains of micro, organisms comprising bacteria and fungi.

Results

The investigation successfully generated a thermodynamically stable o/w type of microemulsion, which exhibited improved transparency and formed a clear solution. Characterization results, including particle size, zeta potential, viscosity, and conductivity measurements, fell within the acceptable range. The therapeutic evaluation demonstrated a substantial enhancement in the in vitro antioxidant, anti-inflammatory, and anti, microbial activity of berberine microemulsion compared to the plain berberine solution.

Conclusion

This study concludes that berberine can be effectively incorporated into a microemulsion system. When topically applied, the microemulsion form exhibits significantly higher therapeutic efficacy against skin diseases compared to the conventional emulsion of berberine.