Nanosuspension Dosage Forms: Product Development & Scale Up

By Jim Huang, PhD, Founder & CEO, Ascendia Pharmaceuticals

Nano-formulation of poorly water-soluble drugs has been proven in commercial products to 1) enhance drug dissolution and oral bioavailability, and 2) increase drug loading and release duration for parenteral drug delivery. Preparation of drug nanosuspensions can be top-down, bottom-up, or a combination of both techniques. This month’s forum will focus on nanosuspensions prepared via the top-down process, ie, wet milling process.

During the nanosuspension formulation development process, efforts should first focus on screening to identify the lead formulation that generates stable nanosuspensions that achieve the desired drug efficacy and pharmacokinetic properties in animals and humans. Thereafter, the nano-milling process should be optimized to determine the critical process parameters with the aid of factorial design during scale up. Finally, consideration should be made in how the nanosuspensions can be incorporated in the final market image dosage form per the desired pharmaceutical product profiles based on the need of patients and available technologies.