Development of Dermal Films Containing Miconazole Nitrate.

Magdalena Bîrsan,Adriana Ciurba,Paula Antonoaea,Aura Rusu,Nicoleta Todoran,Mihai Apostu

doi:10.3390/molecules23071640

Abstract

This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm2, 0.20–0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm2. The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.

Highlights

The development of pharmaceutical forms begins with the preformulation process, which establishes the physical and chemical, pharmaceutical and technological, pharmacological and toxicological features of substances [1]
This study aims to develop new antifungal dermal films based on their mechanical properties and the in vitro availability of miconazole nitrate used as pharmaceutical active ingredient in two variants of concentrations, prepared in the form of two types of polymeric film matrices: hydroxypropyl methylcellulose (HPMC) and hydroxyethyl cellulose (HEC)
The results show that the additional use of 1% HEC in the film composition generates the modification of k1 by 0.06−1, accompanied by a tripling of the amount of miconazole nitrate (MN) that could be released from a film of

Summary

Introduction

The development of pharmaceutical forms begins with the preformulation process, which establishes the physical and chemical, pharmaceutical and technological, pharmacological and toxicological features of substances [1]. In addition to its antifungal activity, MN has an antimicrobial action—the imidazole class, which makes it frequently applied on skin mucosa to heal fungal infections [8]. It inhibits the synthesis of ergosterol, a key component of fungal cell membranes [9]. The development of MN-dermal films can bring various benefits to patients resistant to classical antifungal pharmaceutical forms because this active substance lasts longer in the skin layers, acting as a slow release product

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Conclusion