American Journal of Drug Delivery

, Volume 4, Issue 4, pp 231–247 | Cite as

New developments in topical antifungal therapy

  • Majdeline El Mahrab Robert
  • Yogeshvar N. KaliaEmail author
Review Article


Superficial fungal infections are among the most widespread diseases known to man. They target parts of the body as diverse in form and function as the skin, the nail, the buccal cavity, the eye and the vagina. Fungistatic azole drugs, that is, imidazole- and triazole-containing compounds (e.g. miconazole and itraconazole, respectively), have been the mainstay of antifungal therapy for many years. The polyene nystatin is effective in treating Candida infections but is inactive against cutaneous dermatophytes. The advent of the fungicidal allylamines (e.g. terbinafine) and their congeners (e.g. butenafine) has improved treatment options: the course of therapy is shorter and cure rates higher with fungicidal drugs. Other newer agents include the echinocandins (e.g. caspofungin) that are primarily intended for systemic administration but which may have a role in topical therapy.

In order to elicit a pharmacologic response following topical administration, these agents must enter into and diffuse across the target biologic tissues, which have distinct architectures and compositions depending on their function. The rate and extent of transport will depend on the interplay between the drug’s molecular properties and the characteristics of the biologic tissue. The drug may also interact with specific proteins or other membrane components. These interactions can prolong residence time and therapeutic effect; for example, azoles have an affinity for keratin (as do dermatophytes, their therapeutic target). Drug properties that increase permeability across a given membrane may render the molecule less effective at another biologic tissue; for example, the stratum corneum is a lipidic barrier, whereas the keratin-rich nail contains 10-fold less lipid and is perhaps best viewed as a hydrogel with very low lipid content. Consequently, both offer very different environments and drug delivery challenges compared with the oral and vaginal mucosae. In light of this, it is clear that formulation design and optimization are key steps in increasing the therapeutic efficacy of topical antifungal therapy. Furthermore, the formulation, which is the primary interface with the membrane, must not only be optimized with respect to the drug but also be compatible with the biologic tissue. Thus, developing effective formulations for topical therapy is a complex task. In this review, we provide a brief description of newer approaches in topical antifungal drug development and present a survey of recent work.


Itraconazole Stratum Corneum Caspofungin Micafungin Solid Lipid Nanoparticles 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



Majdeline El Mahrab Robert has a PhD studentship from the University of Geneva. The authors have no conflicts of interest that are directly relevant to the content of this review.


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Copyright information

© Adis Data Informotion BV 2006

Authors and Affiliations

  • Majdeline El Mahrab Robert
    • 1
    • 2
  • Yogeshvar N. Kalia
    • 1
    • 2
    Email author
  1. 1.School of Pharmaceutical SciencesUniversity of Geneva and University of LausanneGenevaSwitzerland
  2. 2.Centre Interuniversitaire de Recherche et d’Enseignement, “Pharmapeptides”ArchampsFrance

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