Ergosta-4,6,8(14),22-tetraen-3-one (
ergone) was isolated from P. umbellatus, which has been demonstrated to possess a variety of pharmacological activities in vivo and in vitro. The purpose of this study was to evaluate the potent
ergone formulations for
cancer chemotherapy, the liposomal formulations were less toxic and provide longer systemic circulation time were selected as candidates of nanocarriers for
ergone. The effect of modification
polyethylene glycol (PEG) on the pharmacokinetics of
liposome showed that the retaining time of
ergone in blood circulation was prolonged by modified PEG. Moreover, the results of pharmacokinetic analysis showed that of PEG
liposome was about 2.8 times higher than that of free PEG
liposome after
intravenous injection into normal rats due to the lower distribution into the reticuloendothelial system tissues. Since PEG
liposome was able to stably encapsulate
ergone in blood, area under plasma concentration-time curve of
ergone was also extensively enhanced after intravenous dosing of
ergone-PEG
liposome into normal rats. In the in vivo studies utilizing solid
tumor-bearing mice, it was confirmed that
ergone-PEG
liposome delivered remarkably larger amount of
ergone to
tumor tissue and provided more significant anti-
tumor activity than free
ergone. In conclusion, PEG
liposome was an effective delivery formulation to achieve increased
ergone release in
tumor and therapeutic efficacy.