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Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Authors Yi, Zhong, Tong, Cao X, Firempong, Liu, Fu, Yang, Feng, Zhang, Xu X, Yu J

Received 3 June 2012

Accepted for publication 11 July 2012

Published 18 September 2012 Volume 2012:7 Pages 5067—5078


Checked for plagiarism Yes

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Chengxue Yi,* Hui Zhong,* Shanshan Tong,* Xia Cao,* Caleb K Firempong, Hongfei Liu, Min Fu, Yan Yang, Yingshu Feng, Huiyun Zhang, Ximing Xu, Jiangnan Yu

Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, People's Republic of China

*These authors contributed equally to this work

Purpose: To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluate the optimum microemulsion prescription, as well as the pharmacokinetics of encapsulated FVS.
Methods: Molecules present in the FVS isolate were identified by gas chromatography/mass spectrometry analysis. The cell viability of FVS was assessed with methyl thiazolyl tetrazolium (MTT) bioassay. Based on the solubility study, phase diagram and stability tests, the optimum prescription of F. velutipes sterol microemulsions (FVSMs) were determined, followed by FVSMs characterization, and its in vivo pharmacokinetic study in rats.
Results: The chemical composition of FVS was mainly ergosterol (54.8%) and 22,23-dihydroergosterol (27.9%). After 72 hours of treatment, both the FVS (half-maximal inhibitory concentration [IC50] = 11.99 µg • mL-1) and the standard anticancer drug, 5-fluorouracil (IC50 = 0.88 µg • mL-1) exhibited strong in vitro antiproliferative activity against SGC cells, with IC50 > 30.0 µg • mL-1; but the FVS performed poorly against LoVo cells (IC50 > 40.0 µg • mL-1). The optimal FVSMs prescription consisted of 3.0% medium chain triglycerides, 5.0% ethanol, 21.0% Cremophor EL and 71.0% water (w/w) with associated solubility of FVS being 0.680 mg • mL-1 as compared to free FVS (0.67 µg • mL-1). The relative oral bioavailability (area-under-the-curve values of ergosterol and 22,23-dihydroergosterol showed a 2.56-fold and 4.50-fold increase, respectively) of FVSMs (mean diameter ~ 22.9 nm) as against free FVS were greatly enhanced.
Conclusion: These results indicate that the FVS could be a potential candidate for the development of an anticancer drug and it is readily bioavailable via microemulsion formulations.

Keywords: Flammulina velutipes sterol, microemulsions, pharmacokinetics, bioavailability

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