Berberine nanostructured lipid carriers by ultrasonication technique: initial study for skin and oral administration

Abstract Berberine (BBR), a natural bioactive ingredient from Eastern nations, has low solubility and permeability that limits its applications. Hence, berberine nanostructured lipid carriers (BBR-NLCs) were fabricated to improve the drug therapeutic effectiveness. Glycerol monostearate, stearic acid and oleic acid were chosen for lipid base whereas Pluronic F127, Span 80, and Transcutol-P were used as the surfactant and co-surfactant. BBR-NLCs had an average particle size of 82 nm, zeta potential of −32 mV, and narrow size distribution (PDI approximately 0.2), prepared with probe ultrasonication at 490 W in 15 min. In addition, BBR-NLCs prepared at optimized conditions showed around 92% of encapsulation efficiency with drug loading over 5.5%. NLCs presented sustained released through mouse skin, dialysis membrane in Franz cell model, and oral dissolution test, compared with free drug over 24 h. Moreover, blank NLCs even increased the cell viability of HaCaT and HEK293T cells at lower concentrations. NLCs significantly enabled higher interactive BBR quantity with investigated cells. Therefore, BBR-NLCs could be considered as a potential nanocarrier for improved bioavailability of this therapeutic agent.