Mucoadhesive Buccal Tablets Based on Chitosan/Gelatin Microparticles for Delivery of Propranolol Hydrochloride

J Pharm Sci. 2015 Dec;104(12):4365-4372. doi: 10.1002/jps.24688. Epub 2015 Oct 27.

Abstract

Propranolol administration through buccal route offers some distinct advantages thanks to the easy access to the oral mucosa, fast onset of action, and avoidance of hepatic and intestinal degradation mechanisms. To overcome the effective removal existing in the buccal cavity, mucoadhesive delivery systems are considered a promising approach as they facilitate a close contact with the buccal mucosa. The aim of this study was to prepare mucoadhesive tablets based on chitosan/gelatin microparticles for buccal delivery of propranolol hydrochloride. Spray-dried microparticles were prepared with different chitosan-gelatin weight ratios and characterized in terms of yield and morphology. Microparticles were subsequently compressed with the drug to obtain loaded buccal tablets. In vitro water uptake, mucoadhesion, release, and permeation tests were performed to investigate tablet ability to hydrate, to adhere to the mucosa, and to deliver drug through buccal mucosa. Microparticles showed a different morphology based on the different chitosan-gelatin weight ratios. Moreover, buccal tablets based on the prepared microparticles showed different technological and functional characteristics in virtue of their composition. In particular, tablets with an excess of chitosan showed the best mucoadhesive properties, allowed the permeation of the greatest drug amount among all formulations, and could be promising for buccal administration of propranolol hydrochloride.

Keywords: buccal; chitosan; drug delivery systems; hydrogels; microparticles; mucoadhesive; spray drying; tablet.

MeSH terms

  • Adhesiveness
  • Administration, Buccal
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Gelatin / chemistry*
  • Microspheres
  • Mouth Mucosa / metabolism*
  • Propranolol / chemistry*
  • Propranolol / metabolism*
  • Swine
  • Tablets / chemistry*
  • Tablets / metabolism*

Substances

  • Drug Carriers
  • Tablets
  • Gelatin
  • Chitosan
  • Propranolol