Positive Health Online

Abstract

SAWANT and COLLEAGUES, Department of Pharmaceutical Sciences and Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Mugar Building, 360 Huntington Avenue, Boston, Massachusetts 02115, USA evaluated the potential of palmitoyl ascorbate (PA)-loaded micelles for ascorbate-mediated cancer cell targeting and cytotoxicity.

Background

The authors sought to evaluate the potential of palmitoyl ascorbate (PA)-loaded micelles for ascorbate-mediated cancer cell targeting and cytotoxicity.

Methodology

PA was incorporated in polyethylene glycol-phosphatidyl ethanolamine micelles at varying concentrations. The formulations were evaluated for PA content by RP-HPLC. A stable formulation was selected based on size and zeta potential measurements. A co-culture of cancer cells and GFP-expressing non-cancer cells was used to determine the specificity of PA micelle binding. In vitro cytotoxicity of the micellar formulations towards various cancer cell lines was investigated using a cell viability assay. To elucidate the mechanism of action of cell death in vitro, the effect of various H(2)O(2) scavengers and metal chelators on PA-mediated cytotoxicity was studied. The in vivo anti-cancer activity of PA micelles was studied in female Balb/c mice bearing a murine mammary carcinoma (4T1 cells).

Results

PA micelles associated preferentially with various cancer cells compared to non-cancer cells in co-culture. PA micelles exhibited anti-cancer activity in cancer cell lines both in vitro and in vivo. The mechanism of cell death was due primarily to generation of reactive oxygen species (ROS).

Conclusion

The anti-cancer activity of PA micelles associated with its enhanced cancer cell binding and subsequent generation of ROS.

References

Sawant RR, Vaze O, D'Souza GG, Rockwell K and Torchilin VP. Palmitoyl ascorbate-loaded polymeric micelles: cancer cell targeting and cytotoxicity. Source Pharmaceutical Research. 28(2): 301-8, Feb 2011.

Comment

The above ground-breaking research, out of the Department of Pharmaceutical Sciences and Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, Massachusetts, is charting the exploration of how micelles with ascorbate (vitamin c) exhibit anti-cancer activity in cancer lines both in vitro and in vivo. Watch this group for the next generation of anti-cancer delivery methodologies.