title: Triggering effect of N-acetylglucosamine on retarded drug release from a lectin-anchored chitosan nanoparticles-in-microparticles system.
abstract: The aim of this study was to investigate the use of N-acetylglucosamine (NAG) to accelerate drug release from a lectin-modified carrier. A wheat germ agglutinin (WGA)-anchored salmeterol xinafoate (SalX)-loaded nanoparticles-in-microparticles system (NiMS) was prepared with an ionotropic gelation technique combined with a spray drying method. The formulated microparticles were spherical, with diameters ranging mainly from 2 to 8 μm; the drug entrapment efficiency was >70% (w/w), and the loading capacity was approximately 8% (w/w). Drug release from WGA-SalX-NiMS, within the first 4h, was approximately 30% less than that from SalX-NiMS, indicating an effect of lectin-modification to retard drug release from the NiMS. Due to "sugar-lectin" interactions, drug release from WGA-SalX-NiMS was substantially increased after the addition of NAG to the release medium. However, no significant influence of NAG was observed on the drug release profile of SalX-NiMS without WGA anchorage. The characteristics of NAG-WGA interaction may provide valuable insights into the "triggering-effects" of specific sugars on drug release from lectin-anchored carriers. These results suggest that it is possible to control drug release from a lectin-anchored drug delivery system using a specific sugar, and that the designed novel WGA-SalX-NiMS may be a suitable formulation for chronotherapy of asthma.
authors.affiliation: Department of Pharmaceutics, Shanghai Eighth People's Hospital, Shanghai 200235, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.forename: Wen-feng
authors.initials: WF
authors.lastname: Dong
authors.forename: Jian-yuan
authors.initials: JY
authors.lastname: Zhou
authors.forename: Xi-ming
authors.initials: XM
authors.lastname: Xu
authors.forename: Feng-qian
authors.initials: FQ
authors.lastname: Li
mesh_terms: D000117:Acetylglucosamine / Q000737:chemistry*; D058666:Adrenergic beta-2 Receptor Agonists / Q000008:administration & dosage / Q000737:chemistry; D000420:Albuterol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems; D008863:Microspheres; D053758:Nanoparticles; D010316:Particle Size; D000068299:Salmeterol Xinafoate; D013997:Time Factors; D014909:Wheat Germ Agglutinins / Q000737:chemistry*
chemical_list: D058666:Adrenergic beta-2 Receptor Agonists; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D014909:Wheat Germ Agglutinins; D000068299:Salmeterol Xinafoate; D048271:Chitosan; D000420:Albuterol; D000117:Acetylglucosamine