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Hydrogel of Ketoconazole and PAMAM Dendrimers: Formulation and Antifungal Activity
- Source :
- Molecules; Volume 17; Issue 4; Pages: 4612-4624, Molecules, Molecules, Vol 17, Iss 4, Pp 4612-4624 (2012)
- Publication Year :
- 2012
- Publisher :
- Molecular Diversity Preservation International, 2012.
-
Abstract
- Ketoconazole (KET), an imidazole derivative with well-known antifungal properties, is lipophilic and practically insoluble in water, therefore its clinical use has some practical disadvantages. The aim of the present study was to investigate the influence of PAMAM-NH2 and PAMAM-OH dendrimers generation 2 and generation 3 on the solubility and antifungal activity of KET and to design and evaluate KET hydrogel with PAMAM dendrimers. It was shown that the surface charge of PAMAM dendrimers strongly affects their influence on the improvement of solubility and antifungal activity of KET. The MIC and MFC values obtained by broth dilution method indicate that PAMAM-NH2 dendrimers significantly (up to 16-fold) increased the antifungal activity of KET against Candida strains (e.g., in culture Candida albicans 1103059/11 MIC value was 0.008 μg/mL and 0.064 μg/mL, and MFC was 2 μg/mL and 32 μg/mL for KET in 10 mg/mL solution of PAMAM-NH2 G2 and pure KET, respectively). Antifungal activity of designed KET hydrogel with PAMAM-NH2 dendrimers measured by the plate diffusion method was definitely higher than pure KET hydrogel and than commercial available product. It was shown that the improvement of solubility and in the consequence the higher KET release from hydrogels seems to be a very significant factor affecting antifungal activity of KET in hydrogels containing PAMAM dendrimers.
- Subjects :
- Antifungal
Dendrimers
Antifungal Agents
medicine.drug_class
Chemistry, Pharmaceutical
Pharmaceutical Science
Microbial Sensitivity Tests
Article
Hydrogel, Polyethylene Glycol Dimethacrylate
Analytical Chemistry
lcsh:QD241-441
chemistry.chemical_compound
lcsh:Organic chemistry
Dendrimer
aqueous solubility
PAMAM dendrimer
ketoconazole
hydrogel
antifungal activity
Drug Discovery
medicine
Imidazole
Organic chemistry
Physical and Theoretical Chemistry
Solubility
Candida albicans
Pamam dendrimers
biology
Organic Chemistry
biology.organism_classification
Ketoconazole
chemistry
Chemistry (miscellaneous)
Self-healing hydrogels
Molecular Medicine
Nuclear chemistry
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Database :
- OpenAIRE
- Journal :
- Molecules; Volume 17; Issue 4; Pages: 4612-4624
- Accession number :
- edsair.doi.dedup.....4fa0a472ecebd4a85c62e7bc3966889b
- Full Text :
- https://doi.org/10.3390/molecules17044612