title: Cetirizine dihydrochloride loaded microparticles design using ionotropic cross-linked chitosan nanoparticles by spray-drying method.
abstract: To control the release rate and mask the bitter taste, cetirizine dihydrochloride (CedH) was entrapped within chitosan nanoparticles (CS-NPs) using an ionotropic gelation process, followed by microencapsulation to produce CS matrix microparticles using a spray-drying method. The aqueous colloidal CS-NPs dispersions with a drug encapsulation efficiency (EE) of <15%, were then spray dried to produce a powdered nanoparticles-in-microparticles system with an EE of >70%. The resultant spherical CS microparticles had a smooth surface, were free of organic solvent residue and showed a diameter range of 0.5~5 μm. The in vitro drug release properties of CedH encapsulated microparticles showed an initial burst effect during the first 2 h. Drug release from the matrix CS microparticles could be retarded by the crosslinking agent pentasodium tripolyphosphate or the wall material. The technique of 'ionotropic gelation' combined with 'spray-drying' could be applicable for preparation of CS nanoparticlesin-microparticles drug delivery systems. CS-NPs based microparticles might provide a potential micro-carrier for oral administration of the freely water-soluble drug--CedH.
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Shanghai 200235, China. fqlijr@gmail.com
authors.forename: Feng-Qian
authors.initials: FQ
authors.lastname: Li
authors.forename: Rui-Rui
authors.initials: RR
authors.lastname: Ji
authors.forename: Xu
authors.initials: X
authors.lastname: Chen
authors.forename: Ben-Ming
authors.initials: BM
authors.lastname: You
authors.forename: Yong-Hua
authors.initials: YH
authors.lastname: Pan
authors.forename: Jia-Can
authors.initials: JC
authors.lastname: Su
mesh_terms: D000284:Administration, Oral; D017332:Cetirizine / Q000008:administration & dosage / Q000737:chemistry*; D048271:Chitosan / Q000737:chemistry*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage / Q000737:chemistry*; D008863:Microspheres; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry; D011208:Powders; D012995:Solubility; D055697:Taste Perception
chemical_list: D005079:Excipients; D039563:Histamine H1 Antagonists, Non-Sedating; D011122:Polyphosphates; D011208:Powders; D048271:Chitosan; C005692:triphosphoric acid; D017332:Cetirizine