title: Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers: Data analysis and modelling.
abstract: In the present study a series of biodegradable and biocompatible poly(ε-caprolactone)/poly(propylene glutarate) (PCL/PPGlu) polymer blends were investigated as controlled release carriers of Risperidone drug (RISP), appropriate for transdermal drug delivery. The PCL/PPGlu carriers were prepared in different weight ratios. Miscibility studies of blends were evaluated through differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Hydrolysis studies were performed at 37°C using a phosphate buffered saline solution. The prepared blends have been used for the preparation of RISP patches via solvent evaporation method, containing 5, 10 and 15wt% RISP. These formulations were characterized using FT-IR spectroscopy, DSC and WAXD in order to evaluate interactions taking place between polymer matrix and drug, as well as the dispersion and the physical state of the drug inside the polymer matrix. In vitro drug release studies were performed using as dissolution medium phosphate buffered saline simulating body fluids. It was found that in all cases controlled release formulations were obtained, while the RISP release varies due to the properties of the used polymer blend and the different levels of drug loading. Artificial Neural Networks (ANNs) were used for dissolution behaviour modelling showing increased correlation efficacy compared to Multi-Linear-Regression (MLR).
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54 124 Thessaloniki, Macedonia, Greece.
authors.forename: Panoraia I
authors.initials: PI
authors.lastname: Siafaka
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54 124 Thessaloniki, Macedonia, Greece.
authors.forename: Panagiotis
authors.initials: P
authors.lastname: Barmpalexis
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54 124 Thessaloniki, Macedonia, Greece.
authors.forename: Maria
authors.initials: M
authors.lastname: Lazaridou
authors.affiliation: Chemistry Department, University of Ioannina, 451 10 Ioannina, Greece.
authors.forename: George Z
authors.initials: GZ
authors.lastname: Papageorgiou
authors.affiliation: Pharmathen S.A, Pharmaceutical Industry, Dervenakion Str 6, 153 51 Athens, Attiki, Greece.
authors.forename: Efthimios
authors.initials: E
authors.lastname: Koutris
authors.affiliation: Pharmathen S.A, Pharmaceutical Industry, Dervenakion Str 6, 153 51 Athens, Attiki, Greece.
authors.forename: Evangelos
authors.initials: E
authors.lastname: Karavas
authors.affiliation: Laboratory of Inorganic Chemical Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54 124 Thessaloniki, Macedonia, Greece.
authors.forename: Margaritis
authors.initials: M
authors.lastname: Kostoglou
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54 124 Thessaloniki, Macedonia, Greece. Electronic address: dbic@chem.auth.gr.
authors.forename: Dimitrios N
authors.initials: DN
authors.lastname: Bikiaris
mesh_terms: D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D065546:Drug Liberation; D005977:Glutarates / Q000737:chemistry; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D008956:Models, Chemical; D016571:Neural Networks, Computer; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D011126:Polypropylenes / Q000737:chemistry; D018967:Risperidone / Q000008:administration & dosage* / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D014150:Antipsychotic Agents; D004337:Drug Carriers; D005977:Glutarates; D011091:Polyesters; D011126:Polypropylenes; C016240:polycaprolactone; D018967:Risperidone
keywords: Blends; Controlled release; Modelling; Poly(propylene glutarate); Poly(ε-caprolactone); Risperidone drug