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.

中文翻译：

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使用混合的聚合物修饰的自纳米乳剂可增强百洛肽的口服生物利用度和生物功效。

磷脂（Ph）是具有广泛生物学特性的天然活性成分。但是，其水溶性差和口服生物利用度低，极大地限制了其在功能性食品和药物中的应用。这项研究旨在探索混合聚合物Pluronic®F127和P123在自纳米乳剂（SNEs）中修饰不同甘油三酸酯（LCT，MCT，SCT）的方法，以增强Ph的口服生物利用度和生物功效。研究，脂解研究，药代动力学研究和抗炎作用。与Ph溶液相比，LCT-Ph-SNE的水溶性提高了3000倍。对SNEs和其他载体（HP-β-CD，PVP）的药代动力学研究表明，LCT-Ph-SNE的生物利用度比未配制的Ph.S.高7.9倍。