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Microparticles of Celecoxib, dispersed in a matrix of poly(lactic-co-glycolic acid) (PLGA), were prepared by electrospraying using different solvent mixtures to investigate the influence upon particle formation and the resulting particle characteristics. Mixtures consisting of a good solvent, acetone, and an anti-solvent, methanol, for PLGA were studied in different ratios. Properties of the spraying solutions were examined and the resulting microparticles were characterized with regard to size, morphology, porosity, solid state form, surface chemistry and drug release. Particle formation was strongly influenced by the polymer molecular conformation during droplet formation and by the anti-solvent concentration during droplet drying. A strong correlation was found between particle morphology and the solubility of the polymer in the solvent mixtures. The lack of chain entanglements in droplets containing anti-solvent resulted in compact polymer conformation and grain-like particle morphology. Further, the early precipitation of polymer and low chain interaction with increasing content of anti-solvent resulted in surface enrichment of drug (from 10 and 20% up to 41 and 57% respectively), also demonstrated by the increasingly higher drug release rates. The results demonstrate the importance of solvent composition in particle preparation and indicate potential for exploiting this dependence to improve pharmaceutical particle design and performance.

Original publication

DOI

10.1007/s10856-015-5379-5

Type

Journal article

Journal

Journal of materials science. Materials in medicine

Publication Date

02/2015

Volume

26

Addresses

Department of Pharmacy, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark, adam.bohr@sund.ku.dk.

Keywords

Sulfonamides, Lactic Acid, Pyrazoles, Polyglycolic Acid, Complex Mixtures, Capsules, Solvents, Materials Testing, Drug Compounding, Diffusion, Electroplating, Particle Size, Surface Properties, Celecoxib