RT Journal Article
SR Electronic
T1 Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes
JF Cancer Biology and Medicine
JO Cancer Biol Med
FD China Anti-Cancer Association
SP 60
OP 75
DO 10.20892/j.issn.2095-3941.2019.0156
VO 17
IS 1
A1 Bingtao Zhai
A1 Qibiao Wu
A1 Wengang Wang
A1 Mingming Zhang
A1 Xuemeng Han
A1 Qiujie Li
A1 Peng Chen
A1 Xiaying Chen
A1 Xingxing Huang
A1 Guohua Li
A1 Qin Zhang
A1 Ruonan Zhang
A1 Yu Xiang
A1 Shuiping Liu
A1 Ting Duan
A1 Jianshu Lou
A1 Tian Xie
A1 Xinbing Sui
YR 2020
UL http://www.cancerbiomed.org/content/17/1/60.abstract
AB Objective: This study aimed to develop a new polyethylene glycol (PEG)ylated β-elemene liposome (PEG-Lipo-β-E) and evaluate its characterization, pharmacokinetics, antitumor effects and safety in vitro and in vivo.Methods: The liposomes were prepared by ethanol injection and high-pressure micro-jet homogenization. Characterization of the liposomes was conducted, and drug content, entrapment efficiency (EE), in vitro release and stability were studied by ultra-fast liquid chromatography (UFLC) and a liquid surface method. Blood was drawn from rats to establish the pharmacokinetic parameters. The anticancer effect was evaluated in a KU-19-19 bladder cancer xenograft model. Histological analyses were performed to evaluate safety.Results: The PEG-Lipo-β-E showed good stability and was characterized as 83.31 ± 0.181 nm in size, 0.279 ± 0.004 in polydispersity index (PDI), −21.4 ± 1.06 mV in zeta potential, 6.65 ± 0.02 in pH, 5.024 ± 0.107 mg/mL in β-elemene (β-E) content, and 95.53 ± 1.712% in average EE. The Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) indicated the formation of PEG-Lipo-β-E. Compared to elemene injection, PEG-Lipo-β-E demonstrated a 1.75-fold decrease in clearance, a 1.62-fold increase in half-life, and a 1.76-fold increase in area under the concentration-time curves (AUCs) from 0 hour to 1.5 hours (P < 0.05). PEG-Lipo-β-E also showed an enhanced anticancer effect in vivo. Histological analyses showed that there was no evidence of toxicity to the heart, kidney, liver, lung or spleen.Conclusions: The present study demonstrates PEG-Lipo-β-E as a new formulation with ease of preparation, high EE, good stability, improved bioavailability and antitumor effects.