Enhanced oral bioavailability and bioefficacy of phloretin using mixed polymeric modified self-nanoemulsions

Phloretin (Ph) is a natural active ingredient with wide biological properties. However, its poor water-solubility and low oral bioavailability limit the application significantly in functional food and drug. This study was to explore the mixed polymer Pluronic® F127 and P123 modified the different triglycerides (LCT, MCT, SCT) in self-nanoemulsions (SNEs) for enhancing the oral bioavailability and bioefficacy of Ph. The SNEs were characterized in terms of physical property study, lipolysis study, pharmacokinetic study, and anti-inflammatory effect. The water-solubility of LCT-Ph-SNE increased 3000-fold compared with Ph solution. Pharmacokinetic study of SNEs and other carriers (HP-β-CD, PVP) results indicated that LCT-Ph-SNE was 7.9-fold more bioavailable compared with unformulated Ph. The anti-inflammatory activity of LCT-Ph-SNE in vivo represented a 6.8-fold enhancement compared with unformulated Ph. This novel SNE formulation may also be used for other poorly soluble ingredients with high loading capacity, which made a significant impact on functional food and drug.