title: Sustained-release of buspirone HCl by co spray-drying with aqueous polymeric dispersions.
abstract: Sustained-release of buspirone HCl (BUH) was attempted by spray drying after dissolving in two commercially available aqueous polymeric dispersions (Eudragit RS 30 D or Kollicoat SR 30 D) at five different drug:polymer ratios (1:1, 1:2, 1:3, 1:6 and 1:9). The produced spray-dried agglomerates were evaluated in terms of their particle size and morphology, production yield, encapsulation efficiency and in-vitro release of BUH. Possible drug-polymer interactions were checked by Differential Scanning Calorimetry (DSC) and FT-IR spectroscopy. Scanning electron microscopy (SEM) was employed for the qualitative characterization of particle size and morphology. Encapsulation efficiency was generally high (around 100%) and independent of the polymeric dispersion type, while production yield was generally low (7.2-31.0%) and significantly lower for the case of Kollicoat SR 30 D (KSR) than for Eudragit RS 30 D (ERS). Scanning electron micrographs showed remarkable changes in size and shape of agglomerates due to the type of aqueous polymeric dispersion and drug:polymer ratio. In-vitro release of BUH from compacted co spray-dried agglomerates was remarkably slower and incomplete for the case of Kollicoat at drug:polymer ratio below 1, presumably due to increased plastic deformation of the developed coating instead of fragmentation in the case of Eudragit coating during compaction.
authors.affiliation: Department of Pharmaceutical Sciences and Pharmaceutics, Applied Science University, Amman, Jordan. nizoubi@yahoo.com <nizoubi@yahoo.com>
authors.forename: Nizar
authors.initials: N
authors.lastname: Al-Zoubi
authors.forename: Hatim S
authors.initials: HS
authors.lastname: Alkhatib
authors.forename: Yasser
authors.initials: Y
authors.lastname: Bustanji
authors.forename: Khaled
authors.initials: K
authors.lastname: Aiedeh
authors.forename: Stavros
authors.initials: S
authors.lastname: Malamataris
mesh_terms: D002065:Buspirone / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D003890:Desiccation; D004339:Drug Compounding; D008855:Microscopy, Electron, Scanning; D011108:Polymers; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water
chemical_list: D003692:Delayed-Action Preparations; C519734:Kollicoat IR; D011108:Polymers; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D017366:Serotonin Receptor Agonists; D014867:Water; C038300:methylmethacrylate-methacrylic acid copolymer; D002065:Buspirone