title: Electrosprayed 4-carboxybenzenesulfonamide-chitosan microspheres for acetazolamide delivery.
abstract: 4-Carboxybenzensulfonamide-chitosan (4-CBS-chitosan) microspheres were prepared by electrospraying with acetazolamide (ACZ) as a model drug. The obtained 4-CBS-chitosan microspheres with or without ACZ-loading were characterized by Fourier transform infrared spectroscopy, differential scanning colorimetry, scanning electron microscopy and particle size analyses. The crystalline form and the stability of ACZ in a basic solution was determined using X-ray single crystal analysis. 4-CBS-chitosan had 90% encapsulation efficiency for ACZ compared to 47% of encapsulation efficiency (EE) obtained from native chitosan, forming 3.1 μm diameter microspheres with a low polydispersity index (0.4). After an initial burst release (58% in 5 min), ACZ-loaded 4-CBS-chitosan gave a sustained release of ACZ (∼ 100% over 3h) in simulated gastric fluid (0.1N HCl; pH 1.2), which was better than that seen for the release from ACZ-loaded chitosan (44% over 1.5h). Thus, 4-CBS-chitosan microspheres are a possible drug carrier in acidic conditions, such as at the gastric mucosal wall.
authors.affiliation: Program of Petrochemistry and Polymer Science, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Phruetchika
authors.initials: P
authors.lastname: Suvannasara
authors.affiliation: Metallurgy and Materials Science Research Institute, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Krisana
authors.initials: K
authors.lastname: Siralertmukul
authors.affiliation: Biomaterials and Bioorganic Chemistry Research Group, Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand. Electronic address: nongnuj.j@chula.ac.th.
authors.forename: Nongnuj
authors.initials: N
authors.lastname: Muangsin
mesh_terms: D000086:Acetazolamide / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D008863:Microspheres; D010316:Particle Size; D013449:Sulfonamides / Q000737:chemistry*
chemical_list: C118985:4-carbobenzoxybenzene sulfonamide; D002257:Carbonic Anhydrase Inhibitors; D004337:Drug Carriers; D013449:Sulfonamides; D048271:Chitosan; D000086:Acetazolamide
keywords: Acetazolamide; Drug delivery carrier; Mucoadhesive chitosan