Physiochemical characterization and pharmacokinetic assessment of Bergamottin solid lipid nanoparticles

Bergamottin (BER) is a natural furocoumarin found in grapefruit juice that inhibits CYP enzymes and has anticancer properties. However, poor solubility and low bioavailability are significant obstacles to use BER as a functional food. No reports are available on the preparation, characterization, and pharmacokinetics of solid lipid nanoparticles of BER. Therefore, this study aims to encapsulate BER in the lipid matrix to increase its solubility and bioavailability. The single emulsification solvent evaporation method was used to prepare the bergamottin solid lipid nanoparticles (BER-SLNs), and their properties were examined using different analytical techniques. Novel HPLC and LC–MS/MS methods were developed. The BER-SLNs mean particle size, zeta potential, and entrapment efficiency were 123.9 ± 4.27 nm, −26.1 ± 2.0, and 83.3 ± 0.30 % respectively. SEM and TEM study confirmed the round and spherical nature of the particles. DSC and PXRD study revealed that the herbal substance is entrapped in the lipid matrix. In-vitro release studies have demonstrated that BER-SLNs exhibit sustained release compared to pure BER. The stability study confirms that the formulation is stable at freezing temperatures. In a cell viability study of BER-SLNs against SH-SY5Y neuroblastoma cells, BER-SLNs have shown good viability up to a concentration of 10 μM, above 85 % of viability obtained in BER-SLNs formulation. The results indicate that BER-SLNs are safe and effective for drug delivery. A pharmacokinetic study of BER-SLNs shows that C_max increases 3.9 times compared to pure BER, 13.16 ± 5.60 ng/mL and 52.16 ± 7.48 ng/mL, respectively. Enhanced bioavailability will open the doors for pharmacodynamics studies.