Solid and Semisolid Innovative Formulations Containing Miconazole-Loaded Solid Lipid Microparticles to Promote Drug Entrapment into the Buccal Mucosa

Risultato della ricerca: Articlepeer review

Abstract

The currently available antifungal therapy for oral candidiasis (OC) has various limita-tions restricting its clinical use, such as short retention time, suboptimal drug concentration and low patients compliance. These issues could be overcome using micro or nanotechnology. In par-ticular, solid lipid microparticles (SLMs) resulted as a particularly promising penetration enhancer carrier for lipophilic drugs, such as the antifungal miconazole (MCZ). Based on these considera-tions, cetyl decanoate (here synthesized without the use of metal catalysis) was employed together with 1-hexadecanol to prepare MCZ-loaded SLMs. These resulted in a powder composed of 45–300 µm diameter solid spherical particles, able to load a high amount of MCZ in the amorphous form and characterized by a melting temperature range perfectly compatible with oromucosal admin-istration (35–37 °C). Moreover, when compared to Daktarin ® 2% oral gel in ex vivo experiments, SLMs were able to increase up to three-fold MCZ accumulation into the porcine buccal mucosa. The prepared SLMs were then loaded into a buccal gel or a microcomposite mucoadhesive buccal film and evaluated in terms of MCZ permeation and/or accumulation into porcine buccal mucosa by using lower doses than the conventional dosage form. The promising results obtained high-lighted an enhancement in terms of MCZ accumulation even at low doses. Furthermore, the pre-pared buccal film was eligible as stable, reproducible and also highly mucoadhesive. Therefore, the formulated SLMs represent a penetration enhancer vehicle suitable to reduce the dose of lipophilic drugs to be administered to achieve the desired therapeutic effects, as well as being able to be ef-fectively embedded into easily administrable solid or semisolid dosage forms.
Lingua originaleEnglish
pagine (da-a)1-23
Numero di pagine23
RivistaPharmaceutics
Volume13
Stato di pubblicazionePublished - 2021

All Science Journal Classification (ASJC) codes

  • ???subjectarea.asjc.3000.3003???

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