A strategy to improve the solubility and bioavailability of the insoluble drug piperlongumine through albumin nanoparticles | [Pakistan Journal of Pharmaceutical Sciences • 2023]

Author(s):

1. Sen Niu: Department of Pharmaceutical Engineering, Xuzhou Pharmaceutical Higher Vocational School of Jiangsu Province,Xuzhou,China

2. Xurui Li: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

3. Zhongqiu Guo: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

4. David Wan: Beijing Rule Biopharma, Co., Ltd.,Beijing,China

5. Yu Liu: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

6. Li Li: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

7. Meng Dong: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

8. Xirong Jia: School of Pharmaceutical Sciences, Liaoning University,Shenyang, Liaoning,China

Abstract:

Piperlongumine (PL) is a biologically active alkaloid derived from peppers, has significant cytotoxic effects on cancer with no cytotoxicity. This study used NabTM technology to prepare PL albumin nanoparticles (PL-BSA-NPs) to improve water solubility and bioavailability. We carried out a pharmacological evaluation of the PL-BSA-NPs. The morphological profile of the PL-BSA-NPs was relatively uniform, with an average particle size of approximately 210 nm, with drug load of 2.1%, and encapsulation rate of 87.6%. PL-BSA-NPs were stable for 4 weeks when stored at 4°C. In vitro release behavior of the PL-BSA-NPs showed a sustained release, with a cumulative release of 67.24% in approximately 24 hours. The pharmacokinetic properties of PL-BSA-NPs were shown that PL-BSA-NPs could maintain a certain level of blood drug concentration for a long time, thus demonstrating the sustained release and increased bioavailability of PL. Finally, we investigated the in vitro antitumor activity of the PL-BSA-NPs and found that PL can significantly inhibit HepG2 cell proliferation, and that PL-BSA-NPs enhanced the inhibitory effect of PL on this proliferative effect. Thus, we concluded that PL can destroy liver cancer cells by increasing ROS levels. These results suggested that PL-BSA-NPs show promising potential as a targeted anti-tumor drug.

Page(s): 483-490

DOI: 10.36721/PJPS.2023.36.2.REG.483-490.1

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 36, Issue: 2, Year: 2023

Keywords:

Pharmacokinetics , antitumor effect , albumin nanoparticles , Piperlongumine , NabTM technology

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