Abstract
Limited bioavailability of green tea polyphenols hampered their delivery to tumor and hence therapeutic effectiveness. This study investigated the antitumor activity of polyphenon-E (PE) encapsulated into chitosan nanoparticles (CSNPs) in Ehrlich solid tumor in mice. CSNPs-PE, with a particle size of 53–69 nm showed 83% entrapment efficiency and a sustained release of PE in pH = 7.4 at 37 °C. The data demonstrated a higher percentage of released drug in case of less crosslinked formulations. Ehrlich ascites carcinoma (EAC) cells (2.5 × 106/0.2 ml/mouse) were injected subcutaneously in the back of mice. Oral administration of CSNPs-PE for 30 days produced a significant decrease in tumor volume (53%) and weight (60%) compared with free PE and voids CSNPs (72%). Compared with free PE and control, cell cycle revealed G0/G1 arrest associated with decrease in proliferating cell nuclear antigen (PCNA). In tumor tissue of CSNPs-PE treated mice, compared with free PE, there were; 1) induction of Bax and p53, 2) activation of caspases-3,-8 and -9, and CD95, 3) decrease in Bcl-2 expression of 4) inhibition of VEGF and CD31 expressions in tumor tissue. In conclusion, encapsulation of PE into CSNPs provided a good platform for cancer chemotherapy and raised existing application of different polyphenols for nanochemotherapy/prevention.
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