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BACKGROUND: Drug-loaded poly(lactide-co-glycolide) particles (100-4500 nm in diameter) were prepared via the electrospraying method. An extensive study was then carried out to determine the parameters affecting the release profile of estradiol (the drug or active pharmaceutical ingredient) in order to facilitate minimum initial burst release of estradiol. RESULTS AND DISCUSSION: The three most important factors affecting estradiol release were identified as: particle size, coating of the particles with chitosan/gelatin and the concentration of the coating agent. It was shown that coating the particles with chitosan significantly reduced the burst and initial release without affecting the subsequent release profile. CONCLUSIONS: This work demonstrates a powerful method of generating drug-loaded polymeric particles with modified release behavior and control over the initial release phase. The surface-modified particles may be useful in controlled therapeutic delivery systems to minimize undesirable side effects.

Original publication

DOI

10.4155/tde.11.154

Type

Journal article

Journal

Ther deliv

Publication Date

02/2012

Volume

3

Pages

209 - 226

Keywords

Chemistry, Pharmaceutical, Chitosan, Coated Materials, Biocompatible, Delayed-Action Preparations, Drug Carriers, Drug Compounding, Estradiol, Gelatin, Kinetics, Lactic Acid, Nanoparticles, Particle Size, Polyglycolic Acid, Polylactic Acid-Polyglycolic Acid Copolymer, Solubility, Surface Properties, Technology, Pharmaceutical