PT  - JOURNAL ARTICLE
AU  - Bingtao Zhai
AU  - Qibiao Wu
AU  - Wengang Wang
AU  - Mingming Zhang
AU  - Xuemeng Han
AU  - Qiujie Li
AU  - Peng Chen
AU  - Xiaying Chen
AU  - Xingxing Huang
AU  - Guohua Li
AU  - Qin Zhang
AU  - Ruonan Zhang
AU  - Yu Xiang
AU  - Shuiping Liu
AU  - Ting Duan
AU  - Jianshu Lou
AU  - Tian Xie
AU  - Xinbing Sui
TI  - Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes
AID  - 10.20892/j.issn.2095-3941.2019.0156
DP  - 2020 Feb 15
TA  - Cancer Biology and Medicine
PG  - 60--75
VI  - 17
IP  - 1
4099  - http://www.cancerbiomed.org/content/17/1/60.short
4100  - http://www.cancerbiomed.org/content/17/1/60.full
SO  - Cancer Biol Med2020 Feb 15; 17
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.