A CONTINUOUS AND SCALABLE BOTTOM-UP PROCESS TO PRODUCE NANOPARTICLE FORMULATIONS FOR ENHANCED DRUG DELIVERY

Abstract

The aim of this study was to develop a process to produce pharmaceutical nanoformulations. A process was designed which can be used as a proof-of-concept at lab scale to mimic a process of continuous liquid antisolvent precipitation followed by immediate (on-line) spray drying. Feasibility studies were carried out on three model drugs (i.e. fenofibrate, budesonide and sodium cromoglicate). Through the proposed process, nanoformulations of two poorly water-soluble drugs (i.e. fenofibrate and budesonide) with lactose or mannitol as the matrix excipient and excipient-free nanoformulation of one water-soluble drug (i.e. sodium cromoglicate) were successfully produced. Characterization and comparison studies confirmed that the nanoformulations of these drugs exhibited much improved dissolution properties and/or enhanced aerosol performance as compared with conventional formulations containing microsized drug particles, indicating the potential of coupling liquid antisolvent precipitation with immediate (on-line) spray drying for the continuous and scalable production of pharmaceutical nanoformulations to achieve enhanced oral/pulmonary delivery.