Enhanced oral bioavailability and prophylactic effects on oxidative stress and hepatic damage of an oil solution containing a rosmarinic acid–phospholipid complex

• RA–phospholipid complex (RA–PLC) and its oil solution were prepared for the first time.
• Partition coefficient and membrane penetration of RA were greatly enhanced by PLC.
• Bioavailability of RA has been greatly enhanced by PLC and its oil solution.
• RA–PLC oil solution showed better antioxidant and hepatoprotective activities.
• PLC oil solution could serve as a viable approach for functional food application.

Rosmarinic acid (RA) is an important naturally occurring polyphenol from plants of the mint family with many health-promoting benefits, but these can be influenced by its poor bioavailability. In this study, the bioavailability and bioefficacy of RA as RA–phospholipid complex (RA–PLC) and as RA–PLC oil solution (RA–PLC–ME) were evaluated. Evaluations in Caco-2 cell monolayers in vitro revealed that the membrane permeability of RA–PLC and RA–PLC–ME was significantly increased (p < 0.05) over that of unformulated RA. Pharmacokinetic studies additionally revealed that RA–PLC and RA–PLC–ME were 1.2- and 2.9-fold more bioavailable than unformulated RA, respectively. Evaluation of bioefficacy in vivo demonstrated that oral administration of RA–PLC–ME produced a greater reduction in the serum levels of AST and ALT (p < 0.05, p < 0.01), and markedly increased antioxidative properties (p < 0.05), compared with unformulated RA. This study indicated that PLC–ME could act as an effective delivery device for RA to enhance oral bioavailability and bioefficacy.

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