Open AccessEnhanced oral bioavailability and bioefficacy of phloretin using mixed polymeric modified self‐nanoemulsions
Author(s) -
Wang Yiling,
Li Dongli,
Lin Huiqiong,
Jiang Sen,
Han Lei,
Hou Shuli,
Lin Shuying,
Cheng Zhefeng,
Bian Wangqing,
Zhang Xinxin,
He Yan,
Zhang Kun
Publication year - 2020
Publication title -
food science and nutrition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.614
H-Index - 27
ISSN - 2048-7177
DOI - 10.1002/fsn3.1637
Subject(s) - bioavailability , chemistry , phloretin , solubility , pharmacokinetics , lipolysis , active ingredient , ingredient , in vivo , drug , chromatography , food science , pharmacology , biochemistry , organic chemistry , microbiology and biotechnology , medicine , adipose tissue , biology
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.