Enhanced oral bioavailability and tissue distribution of a new potential anticancer agent, Flammulina velutipes sterols, through liposomal encapsulation.
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| Abstract |
This study innovatively investigated the anticancer effect of Flammulina velutipes sterols (FVSs), the in vivo pharmacokinetics, and the tissue distribution of FVS-loaded liposomes. The FVS consisting of mainly 54.8% ergosterol and 27.9% 22,23-dihydroergosterol exhibited evident in vitro antiproliferative activity (liver HepG-2, IC50 = 9.3 μg mL(-1); lung A549, IC50 = 20.4 μg mL(-1)). To improve the poor solubility of FVS, F. velutipes sterol liposome (FVSL) was originally prepared. The encapsulation efficiency of ergosterol was 71.3 ± 0.1% in FVSL, and the encapsulation efficiency of 22,23-dihydroergosterol was 69.0 ± 0.02% in FVSL. In comparison to its two free sterol counterparts, the relative bioavailability of ergosterol and 22,23-dihydroergosterol in FVSL was 162.9 and 244.2%, respectively. After oral administration in Kunming mice, the results of tissue distribution demonstrated that the liposomal FVS was distributed mostly in liver and spleen. The drug was eliminated rapidly within 4 h. These findings support the fact that FVS, a potential nutraceutical and an effective drug for the treatment of liver cancer, could be encapsulated in liposomes for improved solubility and bioavailability.
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| Authors | Chengxue Yi, Min Fu, Xia Cao, Shanshan Tong, Qianfeng Zheng, Caleb Kesse Firempong, Xinyi Jiang, Ximing Xu, Jiangnan Yu |
| Journal | Journal of agricultural and food chemistry (J Agric Food Chem) Vol. 61 Issue 25 Pg. 5961-71 (Jun 26 2013) ISSN: 1520-5118 [Electronic] United States |
| PMID | 23721187 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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