Abstract
IntroductionBetamethasone dipropionate is a highly effective corticosteroid anti-inflammatory. However, the main drawback of its topical use is the limited skin penetration into deeper skin layers. Also, its systemic use has shown many side effects.ObjectiveThe goal of this research was to formulate betamethasone dipropionate in nanostructured lipid carriers (NLC) formulae that contain oleic acid to aid its penetration to deeper skin layers and to aid absorption to local regions upon topical application.MethodsNLC formulae were prepared by high shear homogenization then sonication. Formulae were characterized for their particle size, size distribution, electric potential, occlusion factor, entrapment efficiency, drug loading, transmission electron microscopy, in vitro drug release, and ex vivo skin penetration. Compatibility of ingredients with drug was tested using differential scanning calorimetry. Formulae were shown to have appropriate characteristics. NLC formulae were superior to traditional topical formulation in drug release.ResultsUpon testing ex vivo skin penetration, betamethasone dipropionate prepared in NLC formulae was shown to penetrate more efficiently into skin layers than when formulated as a traditional cream. NLC formulation that contained higher percentage of oleic acid showed higher penetration and higher amount of drug to pass through skin.ConclusionIn general, NLC with lower oleic acid percentage was shown to deliver betamethasone dipropionate more efficiently into deeper skin layers while that of a higher oleic acid percentage was shown to deliver the drug more efficiently into deeper skin layers and through the skin, transdermally.
Highlights
Betamethasone dipropionate is a highly effective corticosteroid anti-inflammatory
The goal of this research was to formulate betamethasone dipropionate in nanostructured lipid carriers (NLC) formulae that contain oleic acid to aid its penetration to deeper skin layers and to aid absorption to local regions upon topical application
It was shown that amount of drug that penetrated skin from NLC formulation containing 10 % W/W oleic acid was significantly higher than that of drug suspension, lipid-free formula and/or reference standard formula in comparison. Another interesting finding was that the amount of betamethasone dipropionate that penetrated skin from NLC containing 30% W/W oleic acid was way higher than that of formula containing 10% W/W of oleic acid. These findings suggested that formulation of betamethasone dipropionate in NLC formulae has resulted in increased skin penetration
Summary
Betamethasone dipropionate is a highly effective corticosteroid anti-inflammatory. the main drawback of its topical use is the limited skin penetration into deeper skin layers. Nanoparticles-based drug delivery systems have gained an increased attention in the last decades This took place because nanoparticles have proven to obtain numerous useful characteristics such as controlled release of the drug molecule [1] and penetration enhancement through semipermeable membranes and skin [2]. Amongst the most important lipid-based nanoparticulate drug delivery systems, Nanostructured Lipid Carriers (NLC) arouse as beneficial and highly effective tools for imparting useful properties for drug delivery such as controlled drug release, drug targeting, increased drug stability, high drug payload, enhanced lymphatic transport and increased penetration of stratum corneum [5]. Betamethasone dipropionate, being a corticosteroid, has been widely used as soothing antiinflammatory or immunosuppressant for topical as well as systemic use. The main advantage of betamethasone over other corticosteroids is the lack of retention of sodium and water [8]
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