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Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes
- Source :
- Cancer Biology & Medicine, Vol 17, Iss 1, Pp 60-75 (2020)
- Publication Year :
- 2020
- Publisher :
- China Anti-Cancer Association, 2020.
-
Abstract
- 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.
Details
- Language :
- English
- ISSN :
- 20953941 and 02365251
- Volume :
- 17
- Issue :
- 1
- Database :
- Directory of Open Access Journals
- Journal :
- Cancer Biology & Medicine
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.8cc3e464e06f4a0d91cd02365251ef0c
- Document Type :
- article
- Full Text :
- https://doi.org/10.20892/j.issn.2095-3941.2019.0156