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

Syed Akbar
Hyderabad:  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 thus its medicinal efficacy within eight weeks.

The method, developed by Prof Ashwini Nangia and his team comprising
Jagdish Babu and Palash Sanphui from the School of Chemistry,
University of Hyderabad, will not only increase the shelf life of the
drug up to six months, but also keeps its medicinal properties 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 has some issues
relating to stability. Our method improves the efficacy and aesthetic
appeal of the drug,” Prof Ashwini Nangia told this correspondent.

The major problem with anti brain cancer drugs is its ability to over come the blood-brain barrier. Temozolomide is also prescribed for treatment of skin cancer called melanoma.

They HCU team made solids comprising temozolomide intimately mixed
with an acid, forming so-called 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 suggests that they could be suitable for use in
formulation development, Prof Ashwini 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. The research also revealed that
acids could protect powders of the drug from discoloration and loss of
activity.

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.