title: Enhanced oral bioavailability and tissue distribution of a new potential anticancer agent, Flammulina velutipes sterols, through liposomal encapsulation.
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.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang 212013, People's Republic of China.
authors.forename: Chengxue
authors.initials: C
authors.lastname: Yi
authors.forename: Min
authors.initials: M
authors.lastname: Fu
authors.forename: Xia
authors.initials: X
authors.lastname: Cao
authors.forename: Shanshan
authors.initials: S
authors.lastname: Tong
authors.forename: Qianfeng
authors.initials: Q
authors.lastname: Zheng
authors.forename: Caleb Kesse
authors.initials: CK
authors.lastname: Firempong
authors.forename: Xinyi
authors.initials: X
authors.lastname: Jiang
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
authors.forename: Jiangnan
authors.initials: J
authors.lastname: Yu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001685:Biological Factors / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D055393:Flammulina / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D013261:Sterols / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D001685:Biological Factors; D004337:Drug Carriers; D008081:Liposomes; D013261:Sterols