Performance Evaluation of Pamam Dendrimer Based Clotrimazole Formulations

Clotrimazole (CLTZ) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLTZ is its poor aqueous solubility, which presents a hindrance for the local availability of CLTZ and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 3.5 (G3.5) and generation 4 (G4) with carboxylate (DCC), amine (DCN) and hydroxyl surface groups (DCO) on aqueous solubility, in vitro drug release studies, and for stability studies of CLTZ drug. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLTZ and the more potent were (DCC) dendrimers. The increase in solubility of CLTZ was highest at dendrimer concentration of 10 mg/ml. These observations indicate that PAMAM dendrimers enhance the solubility of CLTZ, The drug dendrimers complexes displayed the controlled release action during in vitro release studies. Formulation with amine and carboxylate were subjected to accelerated stability studies. Key words: poly(amidoamine) dendrimers; clotrimazole; aqueous solubility; surface groups