Drug delivery strategies for improved azole antifungal action

Background. Azole antifungal agents are the most commonly used antifungals in clinical treatment of both superficial and systemic fungal infections. Many azoles are poorly water soluble, which limits their bioavailability and antifungal effects. Objective: To improve the efficacy of azole antifungal drugs by advances in drug delivery. Methods: Manipulation of drug formulations and administration routes to improve the antifungal pharmacokinetics with targeted delivery, rapidly followed by sustained release and prolonged retention of high drug concentration localized at the infection site. Results/conclusion: Formulation and drug delivery strategies can improve the aqueous wetting and dissolution properties by increasing their chemical potential, stabilizing the drug delivery system and targeting high concentration of the azoles to the infection sites, therefore enhancing the bioavailability and therapeutic efficacy of azole antifungals.