Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes

Bingtao Zhai, Qibiao Wu, Wengang Wang, et al


Objective: This study aimed to develop a new polyethylene glycol (PEG)ylated β-elemene liposome (PEG-Lipo-β-E) and evaluate itscharacterization, 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 theliposomes was conducted, and drug content, entrapment efficiency (EE), in vitro release and stability were studied by ultra-fast liquidchromatography (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 evaluatesafety.

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 polydispersityindex (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) indicatedthe formation of PEG-Lipo-β-E. Compared to elemene injection, PEG-Lipo-β-E demonstrated a 1.75-fold decrease in clearance, a1.62-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 evidenceof 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.

Cite this article as: Zhai B, Wu Q, Wang W, Zhang M, Han X, Li Q, et al.Preparation, Characterization, Pharmacokinetics and Anticancer Effectsof PEGylated β-Elemene Liposomes. Cancer Biol Med. 2020; 17: 60-75.doi: 10.20892/j.issn.2095-3941.2019.0156


β-elemene; PEGylated liposome; pharmacokinetics; antitumor effect; bladder cancer

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