title: Electrospun fibers as potential carrier systems for enhanced drug release of perphenazine.
abstract: Solubility represents an important challenge for formulation of drugs, because the therapeutic efficacy of a drug depends on the bioavailability and ultimately on its solubility. Low aqueous solubility is one of the main issues related with formulation design and development of new molecules. Many drug molecules present bioavailability problems due to their poor solubility. For this reason there is a great interest in the development of new carrier systems able to enhance the dissolution of poorly water-soluble drugs. In this work, fibers containing an insoluble model drug and prepared by an electrospinning method, are proposed and evaluated to solve this problem. Two hydrophilic polymers, polyvinylpyrrolidone (Plasdone® K29/32) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) were used to increase the water solubility of perphenazine. The physico-chemical characterization suggests that the drug loaded in the fibers is in the amorphous state. Both polymeric carriers are effective to promote the drug dissolution rate in water, where this active pharmaceutical ingredient is insoluble, due to the fine dispersion of the drug into the polymeric matrices, obtained with this production technique. In fact, the dissolution profiles of the fibers, compared to the simple physical mixture of the two components, and to the reference commercial product Trilafon® 8mg tablets, show that a strong enhancement of the drug dissolution rate can be achieved with the electrospinning technique.
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy. Electronic address: giovanna.bruni@unipv.it.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Bruni
authors.affiliation: Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
authors.forename: Lauretta
authors.initials: L
authors.lastname: Maggi
authors.affiliation: Industrial Engineering Department, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy.
authors.forename: Loredana
authors.initials: L
authors.lastname: Tammaro
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Rosadele Di
authors.initials: RD
authors.lastname: Lorenzo
authors.affiliation: Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
authors.forename: Valeria
authors.initials: V
authors.lastname: Friuli
authors.affiliation: Industrial Engineering Department, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy.
authors.forename: Sharon
authors.initials: S
authors.lastname: D Aniello
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Mariarosa
authors.initials: M
authors.lastname: Maietta
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Vittorio
authors.initials: V
authors.lastname: Berbenni
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Milanese
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Girella
authors.affiliation: C.S.G.I. - Department of Chemistry, Physical-Chemistry Section, University of Pavia, Viale Taramelli 16, 27100 Pavia, Italy.
authors.forename: Amedeo
authors.initials: A
authors.lastname: Marini
mesh_terms: D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D065546:Drug Liberation; D057139:Nanofibers / Q000008:administration & dosage / Q000737:chemistry*; D010546:Perphenazine / Q000008:administration & dosage / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D011145:Polyvinyls / Q000008:administration & dosage / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D011145:Polyvinyls; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D011092:Polyethylene Glycols; D010546:Perphenazine
keywords: Amorphous; Dissolution rate; Electrospinning; Perphenazine; Polymeric drug carrier; Solubility