Polymeric Microspheres for Drug Delivery to the Oral Cavity: An In Vitro Evaluation of Mucoadhesive Potential

Polymeric microparticles were fabricated from Carbopol, polycarbophil, chitosan, or Gantrez using a “water-in-oil emulsification” solvent evaporation method. Mean particle sizes, as determined by laser diffraction, were in the range 23–38 μm. Electron microscopy revealed that all microparticles were...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2003-08, Vol.92 (8), p.1614-1623
Main Authors: Kockisch, Sandra, Rees, Gareth D., Young, Simon A., Tsibouklis, John, Smart, John D.
Format: Article
Language:English
Subjects:
Adhesives - administration & dosage
Adhesives - pharmacokinetics
Animals
bioadhesion
bioavailability
Biological and medical sciences
carbomer
chitosan
Drug Delivery Systems - instrumentation
Drug Delivery Systems - methods
Drug Evaluation, Preclinical
General pharmacology
hydration
Medical sciences
Microspheres
Mouth - drug effects
Mouth - metabolism
mucoadhesion
oral cavity
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polymers - administration & dosage
Polymers - pharmacokinetics
Swine
triclosan
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Summary:Polymeric microparticles were fabricated from Carbopol, polycarbophil, chitosan, or Gantrez using a “water-in-oil emulsification” solvent evaporation method. Mean particle sizes, as determined by laser diffraction, were in the range 23–38 μm. Electron microscopy revealed that all microparticles were spherical and of smooth surface morphology. In pH 7.0 phosphate buffered saline, the microspheres exhibited significantly increased swelling ratios and longer half-times of swelling than the corresponding powdered polymers. The relative merits of the potential usefulness of these microspheres as formulation tools for the enhanced retention of a therapeutic entity within the oral mucosa were evaluated by in vitro mucoadhesion tests. Tensile tests showed that all microspheres under consideration were capable of adhering to porcine esophageal mucosa, with particles prepared from the poly(acrylic acid)s exhibiting greater mucoadhesive strength than those constructed from chitosan or Gantrez. However, in elution experiments involving a challenge with artificial saliva, particles of chitosan or Gantrez were retained onto mucosal tissue for longer time periods than those assembled from the poly(acrylic acid)s. © 2003 Wiley-Liss, Inc. and the American Pharmacists Association
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.10423