The improvement of tyrosol bioavailability by encapsulation into liposomes using pH-driven method.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Tyrosol exhibits poor water solubility and oral bioavailability.
• Effective delivery systems are needed to improve tyrosol's therapeutic potential.

Purpose of the Study:

• To develop and characterize novel tyrosol liposomes (Tyr-LPs) for improved oral delivery.
• To evaluate the physicochemical properties and in vivo pharmacokinetic performance of Tyr-LPs.

Main Methods:

• Liposomes encapsulating tyrosol were prepared using a pH-driven method.
• Characterization involved Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD).
• Physicochemical properties like dispersibility, instability index, polydispersity index (PDI), and encapsulation efficiency (EE) were assessed.
• In vivo pharmacokinetic studies compared oral administration of tyrosol versus Tyr-LPs.

Main Results:

• FTIR and XRD confirmed successful tyrosol encapsulation in an amorphous state within liposomes.
• Optimal dispersibility was achieved with a tyrosol content of 1.33 mg/ml and a Tyr:LP mass ratio of 1:2.
• The optimized Tyr-LP formulation showed an instability index of 0.049 ± 0.004, PDI of 0.274 ± 0.003, and EE of 94.8 ± 2.5%.
• In vivo studies demonstrated a 1.5-fold increase in AUC and a 2.25-fold increase in Cmax for Tyr-LPs compared to free tyrosol.

Conclusions:

• Novel tyrosol liposomes (Tyr-LPs) were successfully prepared, significantly improving tyrosol's oral bioavailability.
• The optimized Tyr-LP formulation offers enhanced dispersibility and encapsulation efficiency.
• This study provides a promising platform for the optimal oral delivery of tyrosol.