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<p>This study focused on the development of a slow-release formulation for artesunate by PEGylated-liposome nanoparticles to improve its pharmacokinetics and antitumor properties on non-small-cell lung cancer (NSCLC) cells. The lipid-film hydration method was used to entrap artesunate in the liposomal nanoformulation coated with DSPE-mPEG(2000). The physical properties of PEGylated liposomal artesunate were characterized by the dynamic light scattering technique. Its drug release, encapsulation efficiency, and pharmacokinetics were evaluated by the HPLC analysis. It effects on the survival and the metastatic activity of NSCLC cells, the A549 cell line, were evaluated. Tumor growth inhibition and survival rate were investigated in BALB/c mice bearing NSCLC. Particle size of the PEGylated liposomal artesunate was in the nano-range (135.8 ± 8.3&#xa0;nm) with a high percentage of encapsulation efficiency (93.08 ± 0.83%). It showed a sustained-release profile providing high bioavailability (T<sub>max</sub>: 15&#xa0;min and C<sub>max</sub>: 166 ± 38.2&#xa0;ng/ml) of artesunate in experimental mice. Pharmacokinetic analysis revealed a 14.5-fold (<i>p</i> &lt; 0.05) increase in AUC<sub>0-24</sub> and prolonged elimination half-life relative to free artesunate. In vitro studies demonstrated an improved cytotoxicity against A549 cells, reducing the IC₅₀ from 59&#xa0;µg/ml and 23&#xa0;µg/ml (free artesunate) to 23.4&#xa0;µg/ml and 11.7&#xa0;µg/ml (liposomal artesunate) at 48&#xa0;h and 72&#xa0;h time points, respectively. In vivo, the liposomal artesunate and free artesunate significantly delayed tumor growth, achieving a tumor growth delay of 45.7% and 18.6% respectively, with a life span prolonged by 30% and 17%, respectively, when compared to the control mice. In conclusion, encapsulation of artesunate in PEGylated liposome nanoparticles increased its bioavailability, which was accompanied by the enhanced anti-tumor activity against NSCLC in vivo.</p> Graphical Abstract <p>Artesunate was encapsulated in the liposome formulation coated with DSPE-PEG (2000), using the lipid-film hydration. The prepared PEGylated liposomal artesunate was characterized by evaluating physical properties, encapsulation efficiency, drug release, and pharmacokinetic properties. The effects of the PEGylated liposomal artesunate on the survival and the metastatic activity as well as the epithelial-mesenchymal transition (EMT) of NSCLC cells were evaluated. The tumor growth inhibition and survival rate were investigated in BALB/c mice bearing NSCLC. In vitro and in vivo investigations indicated that PEGylated nanoliposomal artesunate exerted significantly higher suppressive effects against the growth, migration, and invasion of NSCLC cells compared with free artesunate. PEGylated nanoliposomal artesunate was found to significantly inhibit the EMT process in A549 cells.</p> <p></p>

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Development, characterization, and evaluation of the therapeutic efficacy of PEGylated-nanoliposomal artesunate in mice bearing non-small cell lung carcinoma

  • 期刊论文

  • 发表日期：

    2026年4月15日

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  • Zemin Qin,
  • Xianli Qiao,
  • Ranxin Huang,
  • Junyan Yu

摘要

This study focused on the development of a slow-release formulation for artesunate by PEGylated-liposome nanoparticles to improve its pharmacokinetics and antitumor properties on non-small-cell lung cancer (NSCLC) cells. The lipid-film hydration method was used to entrap artesunate in the liposomal nanoformulation coated with DSPE-mPEG(2000). The physical properties of PEGylated liposomal artesunate were characterized by the dynamic light scattering technique. Its drug release, encapsulation efficiency, and pharmacokinetics were evaluated by the HPLC analysis. It effects on the survival and the metastatic activity of NSCLC cells, the A549 cell line, were evaluated. Tumor growth inhibition and survival rate were investigated in BALB/c mice bearing NSCLC. Particle size of the PEGylated liposomal artesunate was in the nano-range (135.8 ± 8.3 nm) with a high percentage of encapsulation efficiency (93.08 ± 0.83%). It showed a sustained-release profile providing high bioavailability (Tmax: 15 min and Cmax: 166 ± 38.2 ng/ml) of artesunate in experimental mice. Pharmacokinetic analysis revealed a 14.5-fold (p < 0.05) increase in AUC0-24 and prolonged elimination half-life relative to free artesunate. In vitro studies demonstrated an improved cytotoxicity against A549 cells, reducing the IC₅₀ from 59 µg/ml and 23 µg/ml (free artesunate) to 23.4 µg/ml and 11.7 µg/ml (liposomal artesunate) at 48 h and 72 h time points, respectively. In vivo, the liposomal artesunate and free artesunate significantly delayed tumor growth, achieving a tumor growth delay of 45.7% and 18.6% respectively, with a life span prolonged by 30% and 17%, respectively, when compared to the control mice. In conclusion, encapsulation of artesunate in PEGylated liposome nanoparticles increased its bioavailability, which was accompanied by the enhanced anti-tumor activity against NSCLC in vivo.

Graphical Abstract

Artesunate was encapsulated in the liposome formulation coated with DSPE-PEG (2000), using the lipid-film hydration. The prepared PEGylated liposomal artesunate was characterized by evaluating physical properties, encapsulation efficiency, drug release, and pharmacokinetic properties. The effects of the PEGylated liposomal artesunate on the survival and the metastatic activity as well as the epithelial-mesenchymal transition (EMT) of NSCLC cells were evaluated. The tumor growth inhibition and survival rate were investigated in BALB/c mice bearing NSCLC. In vitro and in vivo investigations indicated that PEGylated nanoliposomal artesunate exerted significantly higher suppressive effects against the growth, migration, and invasion of NSCLC cells compared with free artesunate. PEGylated nanoliposomal artesunate was found to significantly inhibit the EMT process in A549 cells.