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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2018, Vol. 23 ›› Issue (11): 1240-1245.doi: 10.12092/j.issn.1009-2501.2018.11.007

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Preparation of piperine liposomes and its antitumor activity of gastric cancer cells in vitro

GUO Li 1, HAN Chenyang 2   

  1. 1 Central Laboratory, 2 Department of Pharmacy, the Second Hospital of Jiaxing,Jiaxing 314001,Zhejiang, China
  • Received:2018-07-09 Revised:2018-09-13 Online:2018-11-26 Published:2018-11-22

Abstract:

AIM: To study the preparation method of piperine liposomes and the mechanism on anti-tumor activity of gastric cancer cells in vitro.  METHODS: Piperine liposomes were prepared by freezing and thawing method. The morphology of liposomes was observed by transmission electron microscopy (TEM). Particle size analyzer and Zeta potential analyzer were used to analyze the particle size and Zeta potential of piperine liposomes, and to investigate the stability of liposomes and the special release of drug in vitro. Human gastric cancer cell MKN45 cells were cultured in vitro and divided into normal group, control group and experimental group. The control group was treated with 50 μmol/L piperine, the experimental group was treated with the liposomes of piperine, the cell viability was detected by CCK-8, the level of apoptosis was detected by flow cytometry, the expression level of apoptosis related protein Bcl-2, Bax, Caspase-3, Caspase-9 was detected by protein immunoblotting, and Hoechst 33342 staining was used to observe the details. RESULTS: The morphology of piperine liposomes was spheroid, the average particle size was (92.32+2.10)nm, and the Zeta potential was(-49.8+3.5)mV. The release rate of piperine liposomes was significantly higher than that of piperine raw material in vitro. The results of cell test showed that the cell viability of the control group and the experimental group was significantly lower than that in the normal group in time dependent manner (P<0.05), the experimental group had statistical significance compared with the control group (P<0.05). The apoptosis rate of the control group and the experimental group was higher than that of the normal group, but the experimental group was significantly higher than that of the control group (P<0.05). The levels of Bcl-2 in the control group and the experimental group were significantly decreased, while the expressions of Bax, Caspase-3 and Caspase-9 were significantly increased. Compared with the normal group, it was statistically significant (P<0.05). CONCLUSION: The release rate of piperine liposomes is higher than that of the drug, which shows that liposomes increase the solubility of piperine, and the ability of piperine liposome to induce MKN45 apoptosis in vitro is higher than that of the drug.

Key words: liposomes, piperine, gastric cancer, antitumor activity

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