Surface and swelling properties of mucoadhesive blends and their ability to release fluconazole in a mucin environment

Colloids Surf B Biointerfaces. 2018 Dec 1:172:586-593. doi: 10.1016/j.colsurfb.2018.09.014. Epub 2018 Sep 6.

Abstract

The aim of this study is to characterize the matrices for the controlled release of fluconazole and to expand the knowledge of their physicochemical properties that influence the process of mucoadhesion. Polymeric carriers of fluconazole were prepared using the following mucoadhesive polymers: Carbopol 974 P NF, Noveon AA-1, HPMC, HEC, chitosan and film-forming polymer Kollidon VA 64. The potential mucoadhesive properties of the polymers and their blends were evaluated by measuring the wettability and then calculating the surface free energy defined by OWRK and vOCG models, determining the polar and dispersion forces, spreading coefficients and work of adhesion of polymers and their blends with fluconazole in the form of tablets. Prepared tablets were characterized by swelling capacity and in vitro drug release to estimate the amount of fluconazole release from selected polymer blends. The study of drug release from selected blends both in simulated saliva fluid (pH = 6.8) and in simulated vaginal fluid (pH = 4.2) containing mucin confirmed the ability of polymeric carriers to continuously deliver drug over a period of about 8 h.

Keywords: In vitro release of fluconazole; Mucin; Surface free energy; Swelling; Wettability; van Oss-Chaudhury-Good model.

MeSH terms

  • Adhesiveness
  • Animals
  • Drug Liberation*
  • Fluconazole / pharmacology*
  • Mucins / chemistry*
  • Polymers / chemistry
  • Swine
  • Tablets
  • Time Factors
  • Wettability

Substances

  • Mucins
  • Polymers
  • Tablets
  • Fluconazole