Paclitaxel-loaded stealth liposomes: Development, characterization, pharmacokinetics, and biodistribution

Abstract

Aim

In the present paper, paclitaxel (PTX)-loaded stealth liposomes were prepared with thin film hydration technique in order to prolong the time of circulation.

Method

The liposomes’ characterization, in vitro release, pharmacokinetics, and biodistribution profile of the drug were investigated.

Results

Microscope showed that the liposomes were spherical in shape with a smooth surface and the size was uniform and appropriate for administration via intravenous injection. The encapsulation efficiency was 91.1 ± 4.3%, and the mean diameter was 82.2 ± 7.6 nm from three batches. The results of in vivo studies indicated that PTX-loaded stealth liposomes show favorable pharmacokinetics and biodistribution compared to the free drug. In comparison with free PTX, the AUC_0-t of PTX liposomes and stealth liposomes increased 1.91- and 3.39-fold, respectively. The stealth liposomes were long-circulating showing a half-life time of 34.2 h against 13.7 h for the conventional ones.

Conclusions

These results suggest that stealth liposomes would serve as a potent PTX delivery vehicle for the future cancer chemotherapy and represent a suitable platform for the development of targeted liposomal PTX systems.

Keywords::

• biodistribution
• long-circulating
• pharmacokinetics
• paclitaxel
• stealth liposomes

Declaration of interest

The authors report no declarations of interest. The authors alone are responsible for the content and writing of the paper.

This work was supported by Dr. Wu Jingyun of Merck for the statistic service in this study.