title: Production of haloperidol-loaded PLGA nanoparticles for extended controlled drug release of haloperidol.
abstract: This study developed an emulsion-solvent evaporation method for producing haloperidol-loaded PLGA nanoparticles with up to 2% (wt/wt. of polymer) drug content, in vitro release duration of over 13 days and less than 20% burst release. The free haloperidol is removed from the nanoparticle suspension using a novel solid phase extraction technique. This leads to a more accurate determination of drug incorporation efficiency than the typical washing methods. It was discovered that PLGA end groups have a strong influence on haloperidol incorporation efficiency and its release from PLGA nanoparticles. The hydroxyl-terminated PLGA (uncapped) nanoparticles have a drug incorporation efficiency of more than 30% as compared to only 10% with methyl-terminated PLGA (capped) nanoparticles. The in vitro release profile of nanoparticles with uncapped PLGA has a longer release period and a lower initial burst as compared to capped PLGA. By varying other processing and materials parameters, the size, haloperidol incorporation and haloperidol release of the haloperidol-loaded PLGA nanoparticles were controlled.
authors.affiliation: Department of Chemical and Biomolecular Engineering, University of Pennsylvania, Philadelphia, PA 19104-6272, USA.
authors.forename: Avinash
authors.initials: A
authors.lastname: Budhian
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Siegel
authors.forename: Karen I
authors.initials: KI
authors.lastname: Winey
mesh_terms: D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D006220:Haloperidol; D019344:Lactic Acid; D036103:Nanotechnology / Q000379:methods*; D043942:Nanotubes; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers
chemical_list: D003692:Delayed-Action Preparations; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D006220:Haloperidol