Triggering effect of N-acetylglucosamine on retarded drug release from a lectin-anchored chitosan nanoparticles-in-microparticles system.

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.
AuthorsHui Li, Wen-feng Dong, Jian-yuan Zhou, Xi-ming Xu, Feng-qian Li
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 449 Issue 1-2 Pg. 37-43 (Jun 5 2013) ISSN: 1873-3476 [Electronic] Netherlands
PMID23587965 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier B.V. All rights reserved.
Chemical References
  • Adrenergic beta-2 Receptor Agonists
  • Delayed-Action Preparations
  • Drug Carriers
  • Wheat Germ Agglutinins
  • Salmeterol Xinafoate
  • Chitosan
  • Albuterol
  • Acetylglucosamine
  • Acetylglucosamine (chemistry)
  • Adrenergic beta-2 Receptor Agonists (administration & dosage, chemistry)
  • Albuterol (administration & dosage, analogs & derivatives, chemistry)
  • Chitosan (chemistry)
  • Delayed-Action Preparations
  • Drug Carriers (chemistry)
  • Drug Compounding
  • Drug Delivery Systems
  • Microspheres
  • Nanoparticles
  • Particle Size
  • Salmeterol Xinafoate
  • Time Factors
  • Wheat Germ Agglutinins (chemistry)

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