title: Microparticles based on chitosan/carboxymethylcellulose polyelectrolyte complexes for colon delivery of vancomycin.
abstract: The aim of this work was to prepare polyelectrolyte complexes based on chitosan (CH) and carboxymethylcellulose (CMC) for colon delivery of vancomycin (VM). Various batches of polyelectrolyte complexes, using three different CH/CMC weight ratios (3:1, 1:1 and 1:3), were prepared and collected as microparticles by spray-drying process. Microparticles were characterized in terms of yield, encapsulation efficiency, drug loading, morphology and mucoadhesion properties. Microparticles water-uptake and VM release as well as its protection against gastric pepsin degradation were also investigated. Finally, the antibacterial activity against Staphylococcus aureus, a Gram-positive model strain, was evaluated. The best formulation CH/CMC 1:3 was selected based on the encapsulation efficiency, water-uptake and drug release rate. Moreover, microparticles were able to prevent VM degradation and showed a good antibacterial activity against S. aureus. Finally, to improve the release of VM in the colon the selected formulation was coated with lauric acid.
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: teresa.cerchiara2@unibo.it.
authors.forename: T
authors.initials: T
authors.lastname: Cerchiara
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Abruzzo
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Parolin
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Vitali
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
authors.forename: F
authors.initials: F
authors.lastname: Bigucci
authors.affiliation: Department of Chemistry and Chemical Technologies, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, CS, Italy.
authors.forename: M C
authors.initials: MC
authors.lastname: Gallucci
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, CS, Italy.
authors.forename: F P
authors.initials: FP
authors.lastname: Nicoletta
authors.affiliation: Department of Pharmacy and Biotechnologies, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Luppi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000378:metabolism; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry; D003106:Colon / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007850:Lauric Acids / Q000737:chemistry; D010434:Pepsin A / Q000378:metabolism; D000071228:Polyelectrolytes / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects; D013499:Surface Properties; D013552:Swine; D014640:Vancomycin / Q000008:administration & dosage* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D007850:Lauric Acids; D000071228:Polyelectrolytes; C030358:lauric acid; D014640:Vancomycin; D048271:Chitosan; D010434:Pepsin A; D002266:Carboxymethylcellulose Sodium
keywords: Carboxymethylcellulose; Chitosan; Colon-specific delivery; Polyelectrolyte complexes; Vancomycin