Preformulation in Drug Research and Pharmaceutical Product Development

Abstract A typical product lifecycle stage is fraught with challenges right from the inception, i.e., early drug discovery/lead optimization to product development. Challenge includes optimization of operation process, i.e., procurement and supply of bulk materials as well as production span to develop a final commercial product. The putative reasons attributed to failure to translation of product from conception to commercialization may include but not limited to subtherapeutic efficacy, toxicity issues, commercial viability, unforeseen operational issues, and so on. Together, these issues may culminate into failures of phase-II and phase-III clinical trials. Hence, to minimize all these formulation and delivery issues during the later stages of product development and registration, there is always a need for preformulation studies before the development stage. Preformulation studies are designed to provide insights of the essential physicochemical attributes of a new chemical entity, drug-excipient compatibility, to determine kinetic rate profile of the drug and the stability indicating assay method. However, the relation between preformulation and pharmacokinetics is also needed to be understood to utilize this concept in a better way. Apart from the general information on preformulation (importance, parameters, technologies, etc.), the chapter also covers a few recent case studies on the role of preformulation in development of dosage forms such as hydrogels, liposomes, and vaccines.