title: In vitro characterization of insulin containing thiomeric microparticles as nasal drug delivery system.
abstract: This study focused on a novel two step preparation method for the generation of insulin containing thiomer microparticles. The first step utilized the interpolymer complexation between poly(vinyl pyrrolidone) (PVP) and poly(acrylic acid) (PAA) or poly(acrylic acid)-cysteine (PAA-Cys), respectively, in the presence of insulin. Thereafter lyophilized coprecipitates were micronized via air jet mill. Particles were evaluated regarding size, morphology, insulin release and the effect on ciliary beat frequency of human nasal epithelial cells in vitro. Results displayed mean particle sizes of 2.6±1.6μm and 2.8±1.7μm for PAA/PVP/insulin and PAA-Cys/PVP/insulin microparticles, respectively, in a range where volitional impaction of particles on nasal epithelium takes place. Multi unit dosage forms showed in addition release for the incorporated insulin and nasal safety as to results of ciliary beat frequency studies (CBF). The introduced jet milled microparticles might in conclusion display a safe nasal insulin drug delivery system leading to improved absorption.
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
authors.forename: Britta
authors.initials: B
authors.lastname: Deutel
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
authors.forename: Flavia
authors.initials: F
authors.lastname: Laffleur
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
authors.forename: Thomas
authors.initials: T
authors.lastname: Palmberger
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
authors.forename: Andreas
authors.initials: A
authors.lastname: Saxer
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
authors.forename: Marlene
authors.initials: M
authors.lastname: Thaler
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria. Electronic address: Andreas.Bernkop@uibk.ac.at.
authors.forename: Andreas
authors.initials: A
authors.lastname: Bernkop-Schnürch
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry*; D000281:Administration, Intranasal; D002478:Cells, Cultured; D002923:Cilia / Q000187:drug effects / Q000502:physiology; D003545:Cysteine / Q000737:chemistry*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004847:Epithelial Cells / Q000187:drug effects / Q000502:physiology; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D007328:Insulin / Q000737:chemistry* / Q000494:pharmacology; D010316:Particle Size; D011205:Povidone / Q000737:chemistry*
chemical_list: D000180:Acrylic Resins; D007004:Hypoglycemic Agents; D007328:Insulin; C006903:carbopol 940; D011205:Povidone; D003545:Cysteine
keywords: CBF; Insulin; Microparticles; Nasal application; Poly(vinyl pyrrolidone); Thiomer