Crystalline nanosuspensions as potential toxicology and clinical oral formulations for BCS II/IV compounds.
Nanosuspensions, formulations based on the reduction of the active pharmaceutical ingredient (API) particle size in the sub-micron range and most typically around 100-200 nm, represent a valuable option for formulators to facilitate oral absorption of Biopharmaceutics Classification System class II and IV compounds. Their ability to increase the API dissolution rate and subsequent absorption and thus oral bioavailability has been demonstrated in preclinical and clinical settings. This review summarizes the current experience in the biopharmaceutic field with the use of nanosuspensions as oral delivery formulations. The principles behind nanosuspensions as well as the in vitro and in silico evaluation are discussed, while examples are presented highlighting both successes as well as limitations in their application as either toxicology or clinical formulations.
Biopharmaceutics, Product Value Enhancement, Pharmaceutical Sciences and Clinical Supply, Merck & Co, Inc, WP75B-210, 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486-0004, USA. filippos.kesisoglou@merck.com
Filippos
F
Kesisoglou
Amitava
A
Mitra
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003460:Crystallization; D016503:Drug Delivery Systems; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D064420:Drug-Related Side Effects and Adverse Reactions; D006801:Humans; D053758:Nanoparticles; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000145:classification; D012995:Solubility; D014116:Toxicology / Q000379:methods
D004364:Pharmaceutical Preparations