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Ocena właściwości reologicznych i mukoadhezyjnych wybranych preparatów z mometazonu furoinianem w postaci aerozolu do nosa

100%
Szymańska E., Winnicka K.
Pediatria i Medycyna Rodzinna
|
2017
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vol. 13
|
issue 2
224-233
EN
Intranasal preparations with mometasone furoate are recognised to be highly efficient and safe in both adults and children. Commercially available nasal sprays are characterised by thixotropic and mucoadhesive properties – factors ensuring effortless drug dosing followed by prolonged retention time in the nasal cavity. Thixotropy and mucoadhesiveness is not a constant value and it is determined by the presence of proper excipients in the preparation’s composition. The aim of the study was to compare rheological and mechanical properties of selected nasal spray formulations with mometasone furoate. In addition, these preparations were investigated for their ex vivo mucoadhesive behaviour to the porcine nasal mucosa. These experiments revealed differences in viscosity and thixotropic properties between nasal sprays depending on the measurement temperature. All analysed preparations possessed mucoadhesive properties in ex vivo conditions. Viscosity and mechanical measurements of the analysed preparations were found to be correlated with the mucoadhesive behaviour in contact with porcine nasal mucosa. An important role of the agitation process on the formulations’ hardness and consistency was also demonstrated.
PL
Preparaty donosowe z mometazonu furoinianem uważane są za wysoce skuteczne i bezpieczne w stosowaniu zarówno u dorosłych, jak i u dzieci. Dostępne aerozole do nosa charakteryzują się właściwościami tiksotropowymi i mukoadhezyjnymi, umożliwiającymi łatwą aplikację leku oraz wydłużającymi czas jego przebywania w jamie nosa. Zdolność do tiksotropii czy mukoadhezji nie jest wielkością stałą, lecz uwarunkowaną obecnością odpowiednich substancji pomocniczych w składzie preparatu. Celem pracy było porównanie właściwości reologicznych i mechanicznych wybranych preparatów z mometazonu furoinianem w postaci aerozolu do nosa. Preparaty te zostały ponadto poddane badaniom właściwości mukoadhezyjnych ex vivo – w tym celu wykorzystano świńską błonę śluzową nosa. W przeprowadzonych doświadczeniach wykazano różnice w lepkości i właściwościach tiksotropowych poszczególnych preparatów w zależności od temperatury pomiaru. Wszystkie analizowane preparaty w warunkach ex vivo charakteryzowały się zdolnością do mukoadhezji. Zaobserwowano zależność między lepkością i strukturą preparatów a ich właściwościami przylegania do świńskiej błony śluzowej nosa. Wykazano istotny wpływ procesu wstrząsania na twardość i spoistość preparatów.
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OLEOGELS AND BIGELS AS TOPICAL DRUG CARRIERS FOR KETOCONAZOLE – DEVELOPMENT AND IN VITRO CHARACTERIZATION

81%
Wróblewska M., Szekalska M., Hafner A., Winnicka K.
Acta Poloniae Pharmaceutica - Drug Research
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2018
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vol. 75
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issue 3
EN
Abstract: The purpose of this study was to develop and characterize novel gel formulations of oleogels and oleo-hydrogels (bigels) as topical drug delivery systems for ketoconazole (KET). Oleogels were prepared using paraffin oil, rapeseed oil or castor oil as a solvent and Aerosil® 200 as organogelator with addition of surfactant Tween 80. Bigels were prepared by mixing castor oil oleogels with sodium alginate hydrogel. The received formulations were analyzed microscopically, for pH, viscosity and the texture profile analysis was also conducted to examine the mechanical parameters. In addition, the in vitro release of KET was evaluated and ex vivo bioadhesive properties of obtained oleogels and bigels on the rat skin model were estimated. It was found that obtained formulations were non-Newtonian systems, showing a shear-thinning behavior and thixotropic properties, with proper textural features such as firmness, compressibility, adhesiveness. Moreover, they were characterized by beneficial bioadhesive properties. Prepared oleogels and bigels were considered as better formulations in terms of drug release compared to commercially available ketoconazole cream.
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