July’s newsletter deals with the drug formulation. In some respects, this area of research represents the Cinderella of drug discovery; it does not capture the headlines occupied by other research fields like gene editing, genetic manipulation, immune therapy and the like. It does, however represent an absolutely essential process in the translation of compounds with interesting activity into candidates for exciting new drugs. I must admit that I was surprised when I first published articles on a drug formulation theme at how heavily downloaded and cited they were. Since then, I have been much less surprised and frequently articles on drug formulation represent some of the most cited articles in Drug Discovery Today. In this month’s newsletter I have featured some of the most interesting articles of the last 6 months. I hope that you will enjoy them and benefit from them whether you are a formulation specialist or not.

The first of two related articles, by Sunil S. Jambhekar and Philip Breen, of LECOM Bradenton School of Pharmacy, Bradenton, Florida, USA and Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR USA  entitled: “Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex” outlines the pivotal position occupied by cyclodextrins, cyclic oligosaccharides capable of interacting with hydrophobic drug substances via the their internal interior. The interaction of drug and cyclodextrin forms a complex that significantly increases the solubility and stability of the parent drug and hence their bioavailability. The review covers the structure and properties of such complexes and, in addition, summarises the regulatory status of drug/cyclodextrin products.  

Following on from this, the second related article, from the same authors, entitled: “Cyclodextrins in pharmaceutical formulations II: solubilization, binding constant, and complexation efficiency” expands upon the first article, focusing upon some the more physicochemical determination related to the solubilization of drug products. They look at the process of complexation and discuss the measurement and significance of binding constants of drug:cyclodextrin complexes. They critically assess complex formation efficiency and those factors that impact upon it. In a more general sense, they analyse the use of cyclodextrins in solid and parenteral dosage forms.

Finally, is the article from Rajesh Thipparaboina, Dinesh Kumar, Rahul B. Chavan and Nalini R. Shastri, of the National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India and School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin entitled: “Multidrug co-crystals: towards the development of effective therapeutic hybrids “. As drug treatment of complex disease moves away from simple monotherapy, the development of drug-drug co-crystal development has represented an important strategy. The reduction in the number of pills or tablets used by a patient, may significantly enhance compliance without enhancing issues related to adverse events or resistance. Moreover, recent successes may suggest that co-crystals may represent an important tool in extending patent position for important drugs. This article deals with many of these topics and highlights the future prospects for therapeutic hybrids, most notably drug-drug, drug-nutraceutical and drug-inorganic salt complexes to improve efficacy and compliance and eventually to represent improved disease management.

Steve Carney was born in Liverpool, England and studied Biochemistry at Liverpool University, obtaining a BSc.(Hons) and then read for a PhD on the Biochemistry and Pathology of Connective Tissue Diseases in Manchester University, in the Departments of Medical Biochemistry and Histopathology. On completion of his PhD he moved to the Kennedy Institute of Rheumatology, London, where he worked with Professor Helen Muir FRS and Professor Tim Hardingham, on the biochemistry of experimental Osteoarthritis. He joined Eli Lilly and Co. and held a number of positions in Biology R&D, initially in the Connective Tissue Department, but latterly in the Neuroscience Department. He left Lilly to take up his present position as Managing Editor, Drug Discovery Today, at Elsevier. Currently, he also holds an honorary lectureship in Drug Discovery at the University of Surrey, UK. He has authored over 50 articles in peer-reviewed journals, written several book chapters and has held a number of patents. Following the West of England Championships the Editor’s band claimed a creditable second place. Probably not enough to get back into the top 200 I’m afraid.