Comparison of the aqueous solubilization of practically insoluble niclosamide by polyamidoamine (PAMAM) dendrimers and cyclodextrins

This study is the first report of the solubilization of niclosamide by cyclodextrin complexation or the interaction between the drug and polyamidoamine (PAMAM) dendrimers. Half generation dendrimers with more polar carboxylate surface functional groups did not increase the solubility of niclosamide....

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Bibliographic Details
Published in:International journal of pharmaceutics 2005-11, Vol.304 (1), p.193-209
Main Authors: Devarakonda, Bharathi, Hill, Ronald A., Liebenberg, Wilna, Brits, Marius, de Villiers, Melgardt M.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Chromatography, High Pressure Liquid
Cyclodextrins
Cyclodextrins - chemistry
Dendrimers
Dissolution
Drug Compounding
Drug Design
Excipients - chemistry
General pharmacology
Kinetics
Medical sciences
Molecular Structure
Niclosamide
Niclosamide - chemistry
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyamines - chemistry
Solubility
Solubilization
Solutions
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Summary:This study is the first report of the solubilization of niclosamide by cyclodextrin complexation or the interaction between the drug and polyamidoamine (PAMAM) dendrimers. Half generation dendrimers with more polar carboxylate surface functional groups did not increase the solubility of niclosamide. From the phase solubility studies, when the fold enhancement in solubility of niclosamide combined with full generation amine terminated PAMAM dendrimers was compared with that obtained when the drug was combined with β- or hydroxypropyl-β-cyclodextrin, the results showed that, except for G-0 dendrimer at pH 7, the solubility of niclosamide was significantly higher in the presence of the dendrimers. In addition, higher equilibrium stability constants and complexation efficiency showed that the dendrimers formed stronger more stable complexes than the CDs. However, the strong interaction between the amine surface functional groups and the niclosamide molecule complexes caused a decrease in dissolution rate compared to the CDs because the interaction retarded the release of the drug from the dendrimers. In addition to increasing the solubility, PAMAM dendrimers therefore also offer the possible for the controlled release of the drug from solid dosage forms.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2005.07.023