Impact of preformulation on drug development.

INTRODUCTION: Preformulation assists scientists in screening lead candidates based on their physicochemical and biopharmaceutical properties. This data is useful for selection of new chemical entities (NCEs) for preclinical efficacy/toxicity studies which is a major section under investigational new drug application. A strong collaboration between discovery and formulation group is essential for selecting right NCEs in order to reduce attrition rate in the late stage development. AREAS COVERED: This article describes the significance of preformulation research in drug discovery and development. Various crucial preformulation parameters with case studies have been discussed. EXPERT OPINION: Physicochemical and biopharmaceutical characterization of NCEs is a decisive parameter during product development. Early prediction of these properties helps in selecting suitable physical form (salt, polymorph, etc.) of the candidate. Based on pharmacokinetic and efficacy/toxicity studies, suitable formulation for Phase I clinical studies can be developed. Overall these activities contribute in streamlining efficacy/toxicology evaluation, allowing pharmacologically effective and developable molecules to reach the clinic and eventually to the market. In this review, the magnitude of understanding preformulation properties of NCEs and their utility in product development has been elaborated with case studies.