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The preparation, characterization of Lupeol PEGylated Liposome and its functional evaluation in vitro as well as pharmacokinetics in rats

Jun Zhang, Huali Liang, Hui Yao, Zhenpeng Qiu, Xinyan Chen, Xixi Hu, Junjie Hu, Guohua Zheng
Drug Development and Industrial Pharmacy 2019 April 3, : 1-25

OBJECTIVE: The objective of this study was to enhance the solubility and bioavailability of Lupeol.

METHODS: Utilizing a thin-film dispersion method, we prepared Lupeol-loaded PEGylated liposomes and Lupeol-loaded liposomes, which was characterized by SEM, mean diameter, PDI, zeta potential and entrapment efficiency(EE). The EE, in vitro release and stability of Lupeol-loaded PEGylated liposomes, were detected by HPLC. In addition to the safety evaluation, the evaluation was carried out on HepG2 cells in vitro; the pharmacokinetics were carried out after i.v. in the rats.

RESULTS: The size, PDI, zeta potential, and EE of Lupeol-loaded PEGylated liposomes and Lupeol-loaded liposomes were 126.9 nm, 0.246, -1.97 mV, 87%; 97.23 nm, 0.25, 1.6 mV, 86.2%, respectively. Lupeol-loaded PEGylated liposomes showed the slow-release effect in vitro release experiments. Lupeol-loaded PEGylated liposomes offered significant advantages over other experimental groups in vitro studies, such as the highest inhibition rate and the highest apoptosis rate. We also found that Lupeol-loaded PEGylated liposomes blocked cells in the G2 M phase. The pharmacokinetics result showed that the AUC of Lupeol-loaded PEGylated liposomes group was 3.2 times higher than free Lupeol group after i.v., the MRT and t1/2 values of Lupeol-loaded PEGylated liposomes (MRT =6.09 h, t1/2 =12.94 h) showed improvements of 2.5 and 4.1 times compared to free Lupeol (MRT= 2.43 h, t1/2 = 3.16 h) .

CONCLUSION: The Lupeol-loaded PEGylated liposomes have successfully solved its poor hydrophilicity, low bioavailability.


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