Improving the therapeutic efficiency of ginger extract for treatment of colon cancer using a suitably designed multiparticulate system

Abstract

Ginger extract (GE), a potential natural anticancer agent, has compromised therapeutic utilization due to poor bioavailability and physicochemical properties. Present study aimed at assigning GE with a pharmaceutical couture so as to improve its biopharmaceutical performance by monitoring its localized (though prolonged) delivery in the distal parts of gastrointestinal tract for the treatment of colon cancer. Alginate beads entrapping 85.9 ± 1.78% GE were subjected to Eudragit S100 coating. Latter is insoluble at acidic and near neutral (6.8) pH of stomach and upper part of small intestine and it led to 50% retardation (upto 12 h) in release of GE. However, it was solubilised at pH > 7.0 resulting in colon targeted system. Developed beads were free flowing, showed a particle size of 0.9 ± 0.006 mm and super class-II release controlled by swelling and polymer relaxation. Preclinical evaluation using 1,2-dimethylhydrazine-induced colon cancer, in male Wistar rats, in terms of histopathology, oxidative stress, mitochondrial complex activity, β-glucuronidase and ammonia concentration determinations indicated GE loaded beads (50 mg/kg) to be significantly better (p < 0.05) than free GE. Highlight of the study was that GE loaded coated alginate beads were administered after the induction of colon cancer and significant recession of the cancers was observed after 4 weeks of treatment.

• Alginate beads
• colon cancer
• dimethylhydrazine
• Eudragit S100
• ginger extract