Abstract

Formulation of Water Insoluble Drugs for IV Injections

Khalid Akhter Ansari, Team Lead, Novartis

The evolving trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and erratic bioavailability due to poor water solubility. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. Because of the clinical demand for new and more efficacious anti-cancer, antiviral, and anti-infective drugs, many of these new drugs must be formulated for injection. Poor water solubility challenges can be overcome by various formulation approaches such as pH manipulation, salt formation, and cosolvent and surfactant addition, or by advance drug delivery techniques such as cyclodextrine complexation, liposomal encapsulation, nanosuspension, lipid drug delivery systems etc. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful injectable drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance.