Formulation of drugs – a key to success

The formulation of drugs by means of drug delivery systems (DDSs) is challenging yet indispensable to ensure efficacy of treatments especially when using drugs that do not present ideal characteristics in terms of stability, safety and pharmaco-dynamics/kinetics. Although many DDSs have reached maturity, resulting in their commercialization for various applications, further investigations and the introduction of new types of delivery carriers are paramount to stimulate and foster this field of science that has become essential to researchers working in both pharmaceutical industries and academia.

Despite the efforts made in the field of drug discovery and design, the optimization of the transport and delivery of drugs to their site of action is often the key to success for a therapy. For this reason, formulation has become of central importance if one has to ensure that a therapeutic compound makes it to the market. The types of DDSs currently in use or under investigation range from lipid-based vessels (liposomes) to polymeric nanoparticles and carbon nanotubes, just to name a few. Formulation technology is also important in finding alternative routes of administration for drugs that are already used in the clinic to ensure a better patient compliance.

In this issue of Drug Discovery Today, Editor’s Choice, I feature four recent papers on the formulation and delivery of drugs. The papers are all available as free downloads, so please have a look at them; I have no doubt you will find them both informative and inspiring.

In my  article entitled “The formulation of polyhedral boranes for the boron neutron capture therapy (BNCT) of cancers”, we review the significant contribution that formulation is making to BNCT. The formulation of boronated compounds can be useful for BNCT to overcome the challenges imposed by biological barriers and target-tissue specificity. Current research on the formulation of polyhedral boranes together with the effort of synthetic chemists in designing new boron-containing pharmacophores may lead BNCT to find its deserved place along other approaches to cancer therapy.

Liposomes are generally the most researched DDSs, which successfully brought many drugs from bench to clinic, especially in the area of cancer therapy. The review by Hank-Jan Guchelaar, Marije Slingerland and Hans Gelderblom offers an overview of the approved liposomal anticancer drugs. In this review the authors also include liposomal drugs at various stages of clinical development and present a discussion on the specific adverse effect associated with the use of liposomes.

Following on from this, Martin Kuentz stresses that the development of lipid-based formulations for the oral delivery of challenging drugs (e.g. lipophilic drugs) requires a systematic, structured approach. The author suggests to initially identify the most promising formulation by checking excipients compatibility, phase behaviour, solubility and dilution, and to subsequently adapt it to the specific requirement of the final dosage form. Case studies in which an enhanced bioavailability of drugs was demonstrated in vivo by using this approach are also presented.

Finally, David Cipolla and Igor Gonda from Aradigm Corp. explore the rationale behind the development of new formulation technologies and inhalation devices to repurpose drugs administered by other routes. This concept can be applied to both local and systemic treatments. Pulmonary drug delivery not only presents advantages in terms of safety and efficacy, but also improves patient compliance, especially when compared with parenteral administration.

I hope that you enjoy reading the articles offered in this newsletter and that these will fuel interest in the stimulating and challenging area of formulation of drugs.


Gianpiero Calabrese was born in Salerno, Italy in 1978 where he completed his MSc in Organic Chemistry at Universita' degli Studi di Salerno. In 2004, he joined the Biomaterials and Drug Delivery Group at University of Portsmouth where he read for a PhD in the “Design, synthesis and preliminary in vitro evaluation of potential agents for Boron Neutron Capture Therapy (BNCT)". In 2008, he joined the Department of Pharmacy at Kingston University, London where he currently is Senior Lecturer in Pharmaceutics. His research interests are mitochondrial targeting in cancer, synthesis of boronated compounds for BNCT, the use of drug delivery systems for the treatment of brain and ophthalmic diseases.

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