RESEARCHERS at the University of Limerick have shown that crystal engineering can improve access to a drug used in the treatment of a tropical disease affecting millions worldwide.
The findings, which could also have a significant impact in making medicine more soluble and palatable for children, have just been published in the Molecular Pharmaceutics journal.
The study investigated the potential benefits of an underexplored crystal engineering strategy to improve the properties of crystalline drugs, which in turn would improve drug absorption in the human system.
The strategy was tested on a drug used for the treatment of schistosomiasis, a tropical disease that affects over 250 million people worldwide.
The Centres for Disease Control and Prevention rates schistosomiasis as second only to malaria as the most devastating parasitic disease.
The research was led by Dr Matteo Lusi, a Lecturer in Crystallography at University of Limerick, who is a researcher in the Bernal Institute in the Faculty of Science and Engineering, along with colleagues in UL, Italy, and Switzerland.
Praziquantel (PZQ) is the drug of choice for the treatment of schistosomiasis but, due to its low solubility and high permeability, a high dose is required particularly in children. This makes it difficult to swallow, which decreases compliance and causes many cases to be untreated.
While smaller dose forms are currently in development, they are considerably more expensive.
“This work demonstrates that a solid solution could increase the solubility of the drug by up to eight times which is key to greater efficacy and reduced side effects for the patients,” Dr Lusi explained.
The results were obtained through a simple crystal modification with relatively low development and manufacturing costs.
“As a proof of principle, we have focused on an essential drug for the treatment of a parasite that is common in tropical and undeveloped countries, many which cannot afford expensive medicines.
“Our approach is also a more general one that can be applied to any crystalline drug forms. This is also critical to achieving UN Sustainable Development grand challenges in good health and wellbeing,” Dr Lusi added.
He said the goal of his research in this area “is to understand how molecules and ions interact in the solid state or crystals and how molecular and ionic interactions translate into tangible chemical and physical properties.
