Concurrent Antisolvent Electrospraying: A Novel Continuous Crystallization Technique.

Pharmaceutical co-crystals (CCs) are multicomponent materials that enable the development of novel therapeutic products by enhancing the properties of active pharmaceutical ingredients, such as solubility, permeability and bioavailability. Currently, CCs are a commercial reality; nonetheless, their industrial production remains a challenge due to problems related to scale up, control and mode of preparation, which usually relies on batch production rather than continuous. This paper describes the implementation of a concurrent coaxial antisolvent electrospray (Co-E), as a new manufacturing technique, for the synthesis of CCs in a rapid, continuous and controlled manner. The features of Co-E were sized against other co-crystallization methods such as antisolvent crystallization, neat and liquid assisted grinding. Three pairs of amino acids were used as model compounds to demonstrate the features of this new system. The Co-E displayed exclusive product characteristics, including spherical particle morphology and enhanced CC formation. This technique exhibited robustness against process disturbances, displaying consistent product characteristics. Co-E represents a new alternative for the reliable production of CCs and other pharmaceutical products.

New solid lipid microparticles for controlled ibuprofen release: formulation and characterization study.

A hot melt dispersion method was used to prepare new sustained release ibuprofen composite microparticles of a solid lipid at ambient temperature, cetyl alcohol. The dispersion of colloidal silicon dioxide nanoparticles (hydrophilic Aerosil 200 or hydrophobic Aerosil R974) either in the oily phase or in the aqueous phase led to the preparation of large (about 400 µm diameter) surfactant free free-flowing particles. Mapping-scanning electronic microscopy using silicon probe revealed that silicon was in the oily core in all cases. The nature of silica nanoparticles and the way used for their dispersion influenced the internal structure of the composite microparticles and the aggregation of nanoparticles in the core of the microparticles. Hydrophobic Aerosil R974 allowed the formation of homogeneous microparticles. Although silica nanoparticles had no influence on thermic profile, crystalline state of ibuprofen and lipid, they had an influence on the kinetics drug release related to the increase of the size of the composite solid lipid microparticles prepared.