Design and fungicidal activity of mucoadhesive lactoferrin tablets for the treatment of oropharyngeal candidosis

Mirjam E. Kuipers, Janette Heegsma, Hester I. Bakker, Dirk Meijer, Pieter J. Swart, Erik W. Frijlink, Anko Eissens, Hillechiena de Vries - Hospers, Jeroen J.M. van den Berg

Research output: Contribution to journalArticleAcademicpeer-review

32 Citations (Scopus)


Lactoferrin (Lf) is a potential drug candidate for the treatment of oropharyngeal Candida infections. However, for an effective therapeutic treatment an appropriate dosage form is required. Therefore a mucoadhesive tablet for buccal application was developed. Tablets of sufficient strength could be produced on high speed tabletting machines, but they could only be obtained when the protein contained at least 7% moisture. The tablet contained sodium alginate both for its release-controlling properties as well as for its mucoadhesive properties. Furthermore, phosphate buffer was added to keep the pH of the saliva in the mouth within the range of 6.5 to 7. 5. In this pH range, Lf has shown to have its highest activity against Candida growth inhibition. The tablet formulation containing Lf had the same antifungal properties as compared with Lf alone, because in most cases identical inhibitory concentrations were observed against several clinical isolates of Candida albicans and Candida glabrata.

In human volunteers the tablets, containing 250 mg Lf and placed in each pouch, were able to keep the Lf concentration in the saliva at effective levels for at least 2 hr, while the pH of the saliva remained within the desired range. We concluded that the developed mucoadhesive tablet can improve the therapeutic efficacy of Lf and that it is suitable for further clinical research.

Original languageEnglish
Pages (from-to)31-38
Number of pages8
JournalDrug Delivery: Journal of Delivery and Targeting of Therapeutic Agents
Issue number1
Publication statusPublished - 13-Feb-2002


  • Buffer
  • Candida
  • Compaction
  • Controlled Drug Release
  • Lactoferrin
  • Mucoadhesion
  • alginic acid
  • buffer
  • lactoferrin
  • phosphate
  • adult
  • article
  • Candida albicans
  • Candida glabrata
  • candidiasis
  • clinical trial
  • controlled clinical trial
  • controlled release formulation
  • controlled study
  • crossover procedure
  • drug delivery system
  • drug design
  • drug dosage form
  • drug effect
  • drug formulation
  • female
  • fungicidal activity
  • fungus culture
  • fungus growth
  • human
  • human experiment
  • in vivo study
  • male
  • minimum inhibitory concentration
  • moisture
  • nonhuman
  • normal human
  • oropharynx
  • pH
  • priority journal
  • saliva
  • skin irritation
  • tablet
  • tablet compression

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