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标题：Poly(amidoamine) Dendrimers Increase Antifungal Activity of Clotrimazole
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作者：Katarzyna Winnicka ; Katarzyna Sosnowska ; Piotr Wieczorek 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2011
卷号：34
期号：7
页码：1129-1133
DOI：10.1248/bpb.34.1129
出版社：The Pharmaceutical Society of Japan
摘要：Clotrimazole (CLO) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLO is its poor aqueous solubility, which presents a hindrance for the local availability of CLO and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 2 (G2) and generation 3 (G3) with amine (PAMAM-NH₂) or hydroxyl surface groups (PAMAM-OH) on aqueous solubility and antifungal activity of CLO were studied. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLO and the more potent were PAMAM-NH₂ dendrimers. The increase in solubility of CLO was highest at dendrimer concentration of 10 mg/ml. Microbiology studies indicated that only PAMAM-NH₂ dendrimers significantly increased the antifungal activity of CLO (a 4—32-fold increase in the antifungal activity compared to pure CLO) and the most potent was dendrimer PAMAM-NH₂ G2. These observations indicate that PAMAM dendrimers might be considered as potential carriers of CLO and provide further impetus to evaluate these polymers for use in basic drug delivery studies and to design semisolid dosage forms based on dendrimers with antimicrobial drugs, like CLO.
关键词：poly(amidoamine) dendrimer;clotrimazole;aqueous solubility;antifungal activity