Merck Research Labs, United States
pp. 68 - 70
Keywords: nanoparticle formulations, drug delivery, solubility
The birth of the nanoparticle (nanos) drug delivery field arguably was seen over 20 years ago with the advent and application of simple oral crystalline nanoparticle formulations. This effective approach for enhancind oral absorption using aqueous suspensions of drug particles milled to sub-micron size is now employed in several marketed drug products. Originally, relatively large amounts of drug were required to make even prototype nano formulations. This made it difficult to investigate nanos in drug discovery space, where available drug quantities are very limited. At Merck research labs, we have developed an innovative new method for generating nanos, using a LabRam® high-frequency resonant mixer. This unique application of a LabRam allows us to prepare nanos at a wide range of scales, from stabilizer high throughput screen quantities in a 96 well plate format to liters. With this capability, we can now evaluate nanos during the drug discovery lead optimization stages all the way to the preparation of long-term toxicology supplies. This lecture describes our new preparation method, which has further applications to other formulation methodologies such as liposomes and nanoemulsions.