Design and fungicidal activity of mucoadhesive lactoferrin tablets for the treatment of oropharyngeal candidosis
Open accessAbstract
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.
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Administration of the glycoprotein lactoferrin can be a valid prospect for C. albicans treatment through sequestration of iron and direct toxicity, and this led to the development of a mucoadhesive tablet containing lactoferrin for treatment of oropharyngeal candidosis.
“Administration of the glycoprotein lactoferrin can be a valid prospect for C. albicans treatment through not only sequestration of iron, but also direct toxicity and this led to the development of a mucoadhesive tablet containing lactoferrin for the treatment of oropharyngeal candidosis (Kuipers et al., 2002; Bai et al., 2006; Velliyagounder et al., 2015).”
From Iron at the Centre of Candida albicans Interactions (2018) · cites this paper as Kuipers et al., 2002
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- Authors
- Kuipers, M. E., Heegsma, J., Bakker, H. I., Meijer, D. K. F., Swart, P. J., Frijlink, E. W., Eissens, A. C., Vries-Hospers, H. G. D., & J. M. van den Berg, J.
- Affiliations
- University of Groningen (NL)
- University Medical Center Groningen (NL)
- ORCID
- Kuipers, Mirjam E.
- Venue
- Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2002-01
- Volume
- 9
- Issue
- 1
- Pages
- 31-38
- ISSN
- 1071-7544 (ISSN-L)
- 1521-0464
- OpenAlex
- W2022877803
- Cited by
- 30
- References
- 22
- Citations by year
- 2025: 1 · 2021: 1 · 2020: 2 · 2019: 1 · 2018: 1 · 2017: 2 · 2016: 1 · 2014: 1 · 2013: 1
- FWCI
- 2.33
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- University of Groningen research database (University of Groningen / Centre for Information Technology) (submittedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- lactoferrin, mucoadhesive tablets, buccal drug delivery, oropharyngeal candidiasis, Candida albicans, Candida glabrata, sodium alginate, antifungal activity, salivary pH, protein stability, tablet formulation
- MeSH terms
- Adhesiveness, Administration, Buccal, Adult, Antifungal Agents, Candida, Candidiasis, Oral, Delayed-Action Preparations, Female, Humans, Hydrogen-Ion Concentration, Lactoferrin, Male, Microbial Sensitivity Tests, Mouth Mucosa, Saliva, Tablets, Drug Design, Cross-Over Studies
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