EARLY-STAGE INSIGHTS FOR DEVELOPING MICONAZOLE-BASED MICROEMULSIONS FOR BUCCAL APPLICATION

The present study covered the development and characterization of microemulsions for buccal delivery of miconazole as a potent antifungal agent with activity in oral candidiasis.In a first attempt, apparent miconazole solubility in different ex cipients (oils, surfactants, cosurfactants) was established, and then, different microemulsions containing oleic acid 5%, Tween 20 40%, polyethylene glycol 400 (PEG 400) 0 -20% and xylitol 5% were prepared using water titration method.The resulting systems were first characterized considering preliminary parameters of pH, conductivity and refractive index, and then analysed with emphasis on droplet size, rheological behaviour, superficial properties and release kinetics.Considering the formulation factors' influence on microemulsion formation, a model system with good characteristics presented Newtonian behaviour, reduced droplet size, hydrophilic character and adequate release, obtained with the maximum concentration of PEG 400 and reduced water content.Conceived as a novel formulation for miconazole delivery, the obtained microemulsion can be further researched as a sprayable or mucoadhesive formulation with potential application in oral candidiasis. RezumatPrezentul studiu a vizat dezvoltarea i caracterizarea unor microemulsii destinate administrrii bucale a miconazolului ca agent antifungic activ n candidoza oral.ntr-o prim etap, a fost stabilit solubilitatea aparent a miconazolului n excipieni diferii (uleiuri, surfactani, cosurfactani), iar apoi diferite microemulsii coninnd acid oleic 5%, Tween 20 40%, polietilenglicol 400 (PEG 400) 0 -20% i xilitol 5% au fost preparate aplicnd metoda titrrii cu faz apoas.Sistemele rezultate au fost iniial caracterizate considernd parametri preliminari de pH, conductivitate i indice de refracie i ulterior analizate din punct de vedere al dimensiunii picturilor, al comportamentului reologic, al proprietilor superficiale i al profilului cinetic.Con sidernd influena factorilor de formulare asupra formrii microemulsiilor, un sistem model cu caracteristici adecvate a prezentat o curgere Newtonian, dimensiune redus a picturilor, hidrofilie crescut i coeficient de difuzie crescut, obinute cu o concentraie maxim a PEG 400 i un coninut redus de ap.Conceput ca o nou formulare pentru eliberarea miconazolului, microemulsia obinut poate fi proiectat ca o formulare spray-abil sau mucoadeziv cu potenial pentru aplicare n cadidoza oral.