Effervescent redispersion of lyophilized polymeric nanoparticles

Background: Freeze-drying is an attractive method for converting nanoparticulate pharmaceutical dispersions into a stable form with a long shelf life. However, practical challenges in translating laboratory practice to the clinic, such as high protectant osmolarity and infeasible reconstitution methods, currently limit lyophilized formulation development of nanoparticle therapeutics. Results: We demonstrate the use of effervescent redispersion for the reconstitution of lyophilized polymeric nanoparticles and we show that a 3:1 mass ratio of effervescent salt produced the optimum redispersibility. With only low-energy hand agitation, reconstitution to sizes less than 600 nm was achieved. Second, the effect of nanoparticle formulation parameters (dispersion concentration, molecular weight of the stabilizing polymer, and physical state of the nanoparticle core) on particle redispersibility were examined. Conclusion: This novel freeze-drying and reconstitution method offers a route to producing redispersible dry powders of nanoparticle therapeutics.