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ISSN 1405-1710 (Print)

2018, Number 1

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Rev Cent Dermatol Pascua 2018; 27 (1)

Comparison of the inhibitory effect on C. albicans, of ketoconazole incorporated in liquid-crystalline mesophases, with that of commercial pharmaceutical forms

Santiago TA, Palma RA, Quirino BCT, Castrillón RLE, Juárez SJJ, Castañeda SJI

Language: Spanish
References: 24
Page: 5-11
PDF size: 267.87 Kb.


ABSTRACT

Introduction: Glycerol monooleate (GMO) is a polar lipid known as a drug permeation enhancer through the skin; its action being explained among other factors, by its interaction with the phospholipid bilayers of the epidermis; which, like the GMO, can exist in different liquid-crystalline mesophases. Previous research has shown that GMO and its derivatives marketed as polyfunctional excipients, are dispersed in water to form liquid nanostructured lyotropic crystalline mesophiles (NCLL) cubic (cubosomes) or hexagonal (hexosomes); thus achieving, due to its similarity with the lipids of the epidermis, increasing the probability of corneal-dermal retention and/or the transdermal absorption of drugs. Objective: Formulate and compare an antifungal agent with topical therapeutic activity with commercial presentations. Material and methods: In this work, nano-sized lyotropic liquid crystals (NCLLs) containing ketoconazole (KTZ) were elaborated, their antifungal effect was evaluated and compared with the effect of KTZ in commercial presentations (200 mg tablets and 2% oral suspension). Results: The NCLLs + KTZ system showed a higher antifungal effect than commercial preparations and due to the relative simplicity of its elaboration, as well as the advantage represented by its topical application design, represents a safer and more effective alternative for the treatment of mycoses with ketoconazole, and other nanometric systems currently under development. Conclusion: A good antifungal potency of ketoconazole was achieved when incorporated into NCLLs (CMI 24 µg/mL KTZ), so that NCLLs are a good option as a drug carrier system.


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