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• W2783605735 abstract "In order to enhance the lipophilicity and thus oral bioavailability of icariin (ICA) and icariside II (ICA II) of total flavonoids of epimedium (TFE), a total flavonoids of epimedium–phospholipid complex (TFE‐PLC) is prepared by wet media milling. The stabilizers Aerosi and SDS are used to formulate TFE‐PLC nanosuspensions (TFE‐PLC–Ns) to improve the dispersion of TFE–PLC. FTIR and DSC data confirms the formation of TFE‐PLC. The oil solubility of ICA and ICA II in the complex in octanol is improved nearly four times over that in TFE. The log P of ICA in TFE‐PLC is significantly increased with a value from 1.61 to 2.02 at pH 4.5, and ICA II, from 3.24 to 4.77. The mean diameter of the TFE‐PLC‐Ns is reduced from 6.166 to 0.424 μm, and its dissolution is improved over TFE. In the in vivo evaluation, TFE‐PLC‐Ns exhibits a considerable enhancement with larger AUC 0–t and shorter T max than TFE and TFE‐PLC. The relative bioavailability of ICA in TFE‐PLC and TFE‐PLC‐Ns are 181.75 and 249.05%, respectively, and for ICA II are 401.63 and 684.70%, respectively. Therefore, it suggests that TFE‐PLC‐Ns has possibilities in enhancing oral bioavailability of TFE, which may be due to its improved lipophilicity and wettability. Practical Applications : The oral bioavailability of ICA and ICA II in TFE are very low due to their poor lipophilicity and cell permeability. Here, TFE‐PLC‐Ns is proposed, which is prepared by wet media milling for improving lipophilic properties and oral bioavailability. In addition, some proofs of TFE‐PLC are investigated in detail, and TFE‐PLC‐Ns significantly increased the oral bioavailability of ICA and ICA II in TFE. Therefore, the authors recommend a potential drug vehicle of TFE‐PLC‐Ns for oral administration of ICA and ICA II, and a novel method of phospholipid complex preparation for industrial manufacture. In this article, the total flavonoids of epimedium–phospholipid complex (TFE‐PLC) is prepared to enhance the lipophilicity of icariin (ICA) and icariside II (ICA II) in TFE. Aerosi and SDS are used to formulate TFE‐PLC nanosuspensions (TFE‐PLC‐Ns) to improve the dispersion of TFE‐PLC. And finally, TFE‐PLC‐Ns exhibits enhanced oral bioavailability of ICA and ICA II compared with them in TFE and TFE‐PLC." @default.
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• W2783605735 date "2018-02-20" @default.
• W2783605735 modified "2023-10-16" @default.
• W2783605735 title "Phospholipid Complex of ICA and ICA II Prepared by Wet Media Milling for Improving Bioavailability" @default.
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• W2783605735 doi "https://doi.org/10.1002/ejlt.201700317" @default.
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