Recent advances and novel strategies in pre-clinical formulation development: an overview.

Preclinical profiling for a New Chemical Entity (NCE), if carried out carefully, can be a good predictor of human clinical outcome. Along with the pre-clinical study design a thorough understanding of the physico-chemical properties of the drug candidate and a careful selection of the formulation development strategy are of high importance. The study scientist can experience various challenges in executing a pre-clinical study. This review article provides an overview of the significance of pre-formulation study parameters and their relevance to preclinical studies. Various physico-chemical properties such as solubility, partition co-efficient, and permeability are attributes critical to the performance of the drug substance. This article presents unique formulation development strategies for the successful completion of pre-clinical studies. Formulation development approach for a pre-clinical study involves taking into consideration various important factors such as duration of the study, Biopharmaceutics Classification System (BCS) of the drug, intended duration of action and the desired route of administration. These parameters play key role in the selection of solubilizers, surfactants, co-solvents and optimum pH for the formulation. Two most common routes of administration in the early screening of pharmaceuticals viz., oral and intravenous are emphasized. The article also describes recent advances in preclinical formulation development including selected examples of in vivo preclinical models for anti-cancer, anti-viral, anti-diabetic and anti-hypertensive drugs. Adherence to the regulatory requirement is also the key to successful completion of the preclinical development. An overview of preclinical formulation development along with basic concepts and the recent studies conducted in the past decade are presented in this review.