title: Spray Dried Chitosan Microparticles for Intravesical Delivery of Celecoxib: Preparation and Characterization.
abstract: Chitosan microparticles containing celecoxib (CB), were developed as chemoprevention of bladder cancer. Furthermore two inclusion complexes of CB with methyl-β-cyclodextrin (C1 and C2) were prepared to improve the solubility of the drug.
  
  
  
  C1 and C2 were obtained by freeze-drying and characterized in the solid state and in solution. Microparticles loaded with CB or C1 or C2 were prepared by spray drying and fully characterized.
  
  
  
  The yield and encapsulation efficiencies of microparticles depended by both the viscosity and the presence of the inclusion complex in the feed medium nebulised. Generally, the microparticles exhibited a spherical shape with mean diameter of approximately 2 μm which was compatible with local intravesical administration using a catheter. The CB release studies from the microparticles allowed us to identify both immediate release systems (microparticles including the complexes) and prolonged release systems (microparticles including CB alone). The latter exhibited good adhesion to the bladder mucosa, as highlighted by a mucoadhesion study. Histological studies revealed a desquamation of the superficial cells when the bladder mucosa was treated with microparticles loaded with CB, while the morphology of the urothelium did not change when it was treated with microparticles loaded with the inclusion complex.
  
  
  
  A new CB intravesical formulation than can easily be administered with a catheter and is able to release the drug at the target site for several hours was realized. This new delivery system could be a good alternative to classic oral CB administration.
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy. angelaassunta.lopedota@uniba.it.
authors.forename: Angela
authors.initials: A
authors.lastname: Lopedota
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.
authors.forename: Annalisa
authors.initials: A
authors.lastname: Cutrignelli
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.
authors.forename: Valentino
authors.initials: V
authors.lastname: Laquintana
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.
authors.forename: Nunzio
authors.initials: N
authors.lastname: Denora
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.|Istituto Tumori IRCCS Giovanni Paolo II, Bari, Italy.
authors.forename: Rosa Maria
authors.initials: RM
authors.lastname: Iacobazzi
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.
authors.forename: Mara
authors.initials: M
authors.lastname: Perrone
authors.affiliation: Department of Chemistry, University of Bari "Aldo Moro", Bari, Italy.|CNR-Institute for Physical and Chemical Processes UOS, Bari, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Fanizza
authors.affiliation: Department of Biology, Section of Animal and Environmental Biology, University of Bari "Aldo Moro", Bari, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Mastrodonato
authors.affiliation: Department of Biology, Section of Animal and Environmental Biology, University of Bari "Aldo Moro", Bari, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Mentino
authors.affiliation: Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, Kansas, USA.
authors.forename: Antonio
authors.initials: A
authors.lastname: Lopalco
authors.affiliation: CNR-Institute for Physical and Chemical Processes UOS, Bari, Italy.
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Depalo
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 4 Orabona Street, 70125, Bari, Italy.
authors.forename: Massimo
authors.initials: M
authors.lastname: Franco
mesh_terms: D000283:Administration, Intravesical; D000818:Animals; D000068579:Celecoxib / Q000008:administration & dosage / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005612:Freeze Drying / Q000379:methods; D008863:Microspheres; D009092:Mucous Membrane / Q000378:metabolism; D010316:Particle Size; D012995:Solubility; D013552:Swine; D001743:Urinary Bladder / Q000378:metabolism; D014783:Viscosity; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D047392:beta-Cyclodextrins; C108732:methyl-beta-cyclodextrin; D048271:Chitosan; D000068579:Celecoxib
keywords: bladder chemoprevention; celecoxib; chitosan spray-dried microparticles; inclusion complex; intravesical formulation