title: Use of mesoporous cellular foam (MCF) in preparation of polymeric microspheres for long acting injectable release formulations of paliperidone antipsychotic drug.
abstract: In this study, high surface area mesoporous silica foam with cellular pore morphology (MCF) was used for injectable delivery of paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. The aim was to enhance paliperidone solubility and simultaneously to prepare long active intractable microspheres. For this reason paliperidone was first loaded in MCF silica, and the whole system was further encapsulated into PLA and PLGA 75/25w/w copolymer in the form of microspheres. It was found that paliperidone, after its adsorption into MCF, was transformed in its amorphous state, thus leading to enhanced in vitro dissolution profile. Furthermore, incorporation of the drug-loaded MCF to polymeric microparticles (PLA and PLGA) prolonged the release time of paliperidone from 10 to 15days.
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Stavroula
authors.initials: S
authors.lastname: Nanaki
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Maria
authors.initials: M
authors.lastname: Tseklima
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Zoe
authors.initials: Z
authors.lastname: Terzopoulou
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Maria
authors.initials: M
authors.lastname: Nerantzaki
authors.affiliation: Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Dimitrios J
authors.initials: DJ
authors.lastname: Giliopoulos
authors.affiliation: Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Konstantinos
authors.initials: K
authors.lastname: Triantafyllidis
authors.affiliation: Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
authors.forename: Margaritis
authors.initials: M
authors.lastname: Kostoglou
authors.affiliation: Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece. Electronic address: dbic@chem.auth.gr.
authors.forename: Dimitrios N
authors.initials: DN
authors.lastname: Bikiaris
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000378:metabolism; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation; D007279:Injections, Subcutaneous; D008863:Microspheres; D000068882:Paliperidone Palmitate / Q000138:chemical synthesis* / Q000378:metabolism; D011060:Poloxalene / Q000138:chemical synthesis / Q000378:metabolism; D011108:Polymers / Q000138:chemical synthesis* / Q000378:metabolism; D016062:Porosity; D012822:Silicon Dioxide / Q000138:chemical synthesis* / Q000378:metabolism; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D011108:Polymers; C464484:pluronic block copolymer P123; D012822:Silicon Dioxide; D011060:Poloxalene; D000068882:Paliperidone Palmitate
keywords: Antipsychotic drug; Long acting injectable; Mesoporous cellular foam (MCF); Microspheres; PLA; PLGA; Paliparidone