In a major research that would benefit brain cancer patients living in tropical regions including India, a team from the University of Hyderabad has developed a method to increase the shelf life and efficacy of anti-cancer drug temozolomide. Temozolomide is the only approved drug in the last two decades for use in chemotherapy to treat aggressive brain tumour called glioblastoma multiforme. This drug, however, is unstable with poor shelf life. It loses colour and medicinal efficacy within eight weeks.
The method, developed by Prof. Ashwini Nangia and his team comprising Jagdi-sh Babu and Palash San-phui from the School of Chemistry, University of Hyderabad, will not only increase the shelf life of the drug up to six months, but also keep its medicinal pro-perties intact for effective treatment of brain cancer. “Temozolomide reacts in tropical climate and this causes the drug to lose colour. It also loses its medicinal activity. For patients, it is disturbing to see a dark tablet. The formulation of the drug has some issues relating to stability. Our method improves the efficacy and aesthetic appeal of the drug,” Prof. Nangia said.
The HCU team thoroughly mixed solids comprising temozolomide with an acid, forming pharmaceutical co-crystals. The acid effectively protects the drug from degradation, and the co-crystals showed no signs of discoloration for over six months, even in humid air. Preliminary assessment of the pharmacological properties of the co-crystals suggest that they could be suitable for use in formulation development, Prof. Nangia said. “In drug development, the efficacy of the active drug ingredient is important, but proper formulation is also essential to ensure that the administered drug acts as it should. Our research also revealed that acids could protect powders of the drug from discoloration and loss of activity,” he explained.
Temozolomide is stable in the presence of acid, but when white tablets of the drug are stored for an extended period, they turn light pink or tan. This discoloration is indicative of degradation by water in neutral or basic conditions, which lowers the effectiveness of the drug, and has the potential to disconcert patients. Temozolomide is also prescribed for treatment of skin cancer melanoma.