title: In vitro and in vivo evaluation of albumin-encapsulated primaquine diphosphate prepared by nebulization into heated oil.
abstract: Nebulization of an aqueous mixture of primaquine diphosphate and albumin into heated vegetable oil produces spherical particles with an average size of 6 microm. The microparticles are relatively stabile in buffers of pH 7.2 and 4.5 and completely degrade when exposed to proteolytic enzymes such as trypsin. Pharmacokinetic evaluation of the albumin-encapsulated primaquine diphosphate shows significantly higher levels in mouse liver tissue relative to free drug 2-48 h post-IP administration. Higher AUC (2.8x), lower steady-state volume of distribution (10x) and slower half-life (2.5x) relative to an equivalent dose of free primaquine diphosphate suggest liver targeting and sustained release of the drug from the microparticles.
authors.affiliation: Division of Parasitic Diseases, National Center of Infectious Diseases, Centers for Disease Control and Prevention, Atlanta, GA 30333, USA.
authors.forename: M D
authors.initials: MD
authors.lastname: Green
authors.forename: M J
authors.initials: MJ
authors.lastname: D'Souza
authors.forename: J M
authors.initials: JM
authors.lastname: Holbrook
authors.forename: R A
authors.initials: RA
authors.lastname: Wirtz
mesh_terms: D000418:Albumins; D000818:Animals; D000962:Antimalarials / Q000493:pharmacokinetics*; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods; D008099:Liver / Q000378:metabolism; D051379:Mice; D008863:Microspheres; D010938:Plant Oils; D011319:Primaquine / Q000493:pharmacokinetics*
chemical_list: D000418:Albumins; D000962:Antimalarials; D004337:Drug Carriers; D010938:Plant Oils; D011319:Primaquine