title: Solid dispersions of imidazolidinedione by PEG and PVP polymers with potential antischistosomal activities.
abstract: Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble drugs. The increase of the dissolution rate presented by (5Z)-3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (LPSF/FZ4) from the solid dispersions is related to the existence of intermolecular interactions of hydrogen bond type (>N-H···O<) between the amide group (>N-H) of the LPSF/FZ4 and the ether group (-O-) of the polyethyleneglycol polymer, or the carbonyl (C=O) of the polyvinylpyrrolidone polymer (PVP). The intensity of these interactions is directly reflected in the morphology acquired by LPSF/FZ4 in these systems, where a new solid phase, in the form of amorphous aggregates of irregular size, was identified through scanning electron microscopy and confirmed in the characterizations achieved using X-ray diffraction and thermal analysis of DSC. The solid dispersions with the polymer PVP, in higher concentrations, were revealed to be the best option to be used in the formulations of LPSF/FZ4 in both theoretical and experimental studies.
authors.affiliation: Laboratório de Tecnologia dos Medicamentos, UFPE, Recife, Brazil.
authors.forename: Francimary L
authors.initials: FL
authors.lastname: Guedes
authors.forename: Boaz G
authors.initials: BG
authors.lastname: de Oliveira
authors.forename: Marcelo Z
authors.initials: MZ
authors.lastname: Hernandes
authors.forename: Carlos A
authors.initials: CA
authors.lastname: De Simone
authors.forename: Francisco J B
authors.initials: FJ
authors.lastname: Veiga
authors.forename: Maria do Carmo A
authors.initials: Mdo C
authors.lastname: de Lima
authors.forename: Ivan R
authors.initials: IR
authors.lastname: Pitta
authors.forename: Suely L
authors.initials: SL
authors.lastname: Galdino
authors.forename: Pedro José Rolim
authors.initials: PJ
authors.lastname: Neto
mesh_terms: D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D006827:Hydantoins / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012556:Schistosomicides / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility
chemical_list: C562232:3-(4-chlorobenzyl)-5-(4-nitrobenzylidene)imidazolidine-2,4-dione; D004304:Dosage Forms; D004337:Drug Carriers; D006827:Hydantoins; D011108:Polymers; D012556:Schistosomicides; D011092:Polyethylene Glycols; D011205:Povidone