Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes. - GreenMedInfo Summary
Preparation, characterization, pharmacokinetics and anticancer effects of PEGylatedβ-elemene liposomes.
Cancer Biol Med. 2020 02 15 ;17(1):60-75. PMID: 32296587
Bingtao Zhai
This study aimed to develop a new polyethylene glycol (PEG)ylatedβ-elemene liposome (PEG-Lipo-β-E) and evaluate its characterization, pharmacokinetics, antitumor effects and safetyand.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),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.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 (<0.05). PEG-Lipo-β-E also showed an enhanced anticancer effect. Histological analyses showed that there was no evidence of toxicity to the heart, kidney, liver, lung or spleen.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.