Abstract
Insufficient aqueous solubility of clotrimazole (CLO) is the main problem in designing pharmaceutical formulations and limits its therapeutic efficiency. Polyamidoamine (PAMAM) dendrimers give the opportunity to decrease this limitation because of their solubilising and permeation enhancement properties. The aim of this study was to examine the influence of PAMAM dendrimers on the release of CLO from hydrogels and water suspensions. PAMAM dendrimers improved permeation of CLO from all analyzed formulations in the following order: PAMAM-NH2 G3 > PAMAM-NH2 G2 > PAMAM-OH G3 > PAMAM-OH G2. The effect evoked by PAMAM dendrimers was the most potent from hydrogels containing dissolved drug. Key words: Polyamidoamine (PAMAM) dendrimers, clotrimazole, hydrogels.
Highlights
Clotrimazole (CLO) is a local imidazole-derivative antifungal agent that is used for the treatment of skin and vaginal infections caused by various species of pathogenic dermatophytes and yeasts (Holt, 1974; Henry et al, 2000)
In order to improve the cutaneous penetration in dermal preparations, chemical enhancers are used (Pathan and Setty, 2009), which increase active substance's solubility in the vehicle, improve the partition coefficient or modify barrier properties of stratum corneum
The membrane permeability of drug depends on its solubility and stratum corneum/vehicle partition coefficient (Michaels et al, 1975)
Summary
Clotrimazole (CLO) is a local imidazole-derivative antifungal agent that is used for the treatment of skin and vaginal infections caused by various species of pathogenic dermatophytes and yeasts (Holt, 1974; Henry et al, 2000). An optimal therapeutic effect of dermal drug depends on the appropriate dosage system, physicochemical properties of the substance, type of vehicle (lipophilic, hydrophilic) and the presence of skin absorption enhancers, which influence diffusion of a medical agent from vehicle to skin. One of the most examined families of dendrimers is polyamidoamine (PAMAM) dendrimers, which are being investigated as permeation enhancer and carriers for several routes of delivery: transdermal, oral, ocular or even intravenous (Cheng et al, 2007a; Borowska et al, 2012). The aim of this work was to examine the influence of concentration and type of surface groups of PAMAM dendrimers generation 2 and 3 (G2, G3) on in vitro release of CLO. In two molecular states and from water suspensions were studied
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