title: Controlled release from drug microparticles via solventless dry-polymer coating.
abstract: A novel solvent-less dry-polymer coating process employing high-intensity vibrations avoiding the use of liquid plasticizers, solvents, binders, and heat treatments is utilized for the purpose of controlled release. The main hypothesis is that such process having highly controllable processing intensity and time may be effective for coating particularly fine particles, 100 μm and smaller via exploiting particle interactions between polymers and substrates in the dry state, while avoiding breakage yet achieving conformal coating. The method utilizes vibratory mixing to first layer micronized polymer onto active pharmaceutical ingredient (API) particles by virtue of van der Waals forces and to subsequently mechanically deform the polymer into a continuous film. As a practical example, ascorbic acid and ibuprofen microparticles, 50-500 μm, are coated with the polymers polyethylene wax or carnauba wax, a generally recognized as safe material, resulting in controlled release on the order of seconds to hours. As a novelty, models are utilized to describe the coating layer thickness and the controlled-release behavior of the API, which occurs because of a diffusion-based mechanism. Such modeling would allow the design and control of the coating process with application for the controlled release of microparticles, particularly those less than 100 μm, which are difficult to coat by conventional solvent coating methods.
authors.affiliation: Otto H. York Department of Chemical, Biological, and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark, New Jersey, 07102.
authors.forename: Maxx
authors.initials: M
authors.lastname: Capece
authors.forename: Jason
authors.initials: J
authors.lastname: Barrows
authors.forename: Rajesh N
authors.initials: RN
authors.lastname: Davé
mesh_terms: D001205:Ascorbic Acid / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004058:Diffusion; D007052:Ibuprofen / Q000737:chemistry*; D007700:Kinetics; D008956:Models, Chemical; D010316:Particle Size; D011095:Polyethylenes / Q000737:chemistry*; D012995:Solubility; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D014885:Waxes / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D011095:Polyethylenes; D014885:Waxes; D001205:Ascorbic Acid; C026344:carnauba wax; D007052:Ibuprofen
keywords: Coating; Diffusion; Dissolution; controlled release; dry-polymer coating; microparticles; ordered mixture; solvent-less coating; vibratory mixing