Alginate Oligosaccharides Affect Mechanical Properties and Antifungal Activity of Alginate Buccal Films with Posaconazole

Mar Drugs. 2019 Dec 9;17(12):692. doi: 10.3390/md17120692.

Abstract

Sodium alginate and its oligosaccharides through potential antifungal properties might improve the activity of antifungal drugs enhancing their efficacy and potentially reducing the frequency of application. Mucoadhesive buccal films are oral dosage forms designed for maintaining both local or systemic drug effects and seem to be a very promising alternative to conventional oral formulations. Hence, in this study, mucoadhesive buccal films based on the alginate and its oligosaccharide oligomer composed predominantly of mannuronic acid for the administration of posaconazole-antifungal drug from the azole group were developed. As the polymer gelation method, a relatively new freeze-thaw technique was chosen. All prepared formulations were examined for pharmaceutical tests, swelling, mechanical, and mucoadhesive properties. In addition, the influence of sodium alginate (ALG) and alginate oligosaccharides (OLG) on POS antifungal activity on Candida species was performed. It was observed that film formulation containing 1% ALG and 1% OLG (F2) was characterized by optimal mucoadhesive and swelling properties and prolonged drug release up to 5 h. Additionally, it was shown that OLG affected the growth reduction of all tested Candida spp. The obtained data has opened the way for future research for developing OLG-based dosage forms, which might increase the activity of antifungal drugs.

Keywords: alginate; alginate oligosaccharides; antifungal activity; buccal films; freeze-thaw technique; posaconazole.

MeSH terms

  • Adhesiveness
  • Administration, Buccal
  • Alginates / chemistry*
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / pharmacology
  • Candida / drug effects
  • Chemistry, Pharmaceutical
  • Drug Delivery Systems
  • Drug Liberation
  • Mouth Mucosa / metabolism
  • Oligosaccharides / chemistry*
  • Polymers / chemistry
  • Triazoles / administration & dosage*
  • Triazoles / pharmacology

Substances

  • Alginates
  • Antifungal Agents
  • Oligosaccharides
  • Polymers
  • Triazoles
  • posaconazole