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首页> 外文期刊>Clinical and experimental allergy : >Dissolution in nasal fluid, retention and anti-inflammatory activity of fluticasone furoate in human nasal tissue ex vivo.
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Dissolution in nasal fluid, retention and anti-inflammatory activity of fluticasone furoate in human nasal tissue ex vivo.

机译：离体在人鼻组织中糠酸氟替卡松在鼻液中的溶解，保留和消炎活性。

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BACKGROUND: Intranasal glucocorticoids represent the most effective pharmacologic treatment of allergic rhinitis. So far, no clinical data are available that compare fluticasone furoate (FF) with other intranasally applied glucocorticoids. OBJECTIVE: Because the pharmacokinetic behaviour of drugs governs their presence at the therapeutic target site we analysed selected in vitro properties of FF in comparison with triamcinolone acetonide (TCA), budesonide (Bud), fluticasone propionate (FP) and mometasone furoate (MF). Additionally, we determined the anti-inflammatory activity of the glucocorticoid fraction residing in human nasal tissue samples after washing. METHODS: We analysed the solubility of the compounds in artificial human nasal fluid and the retention in human nasal tissue as well as typical spray volumes of commercially available drug preparations. As an anti-inflammatory measure, we evaluated the inhibition of IL-8 release from epithelial cells. RESULTS: FF is delivered in the smallest application volume per spray. Despite the low aqueous solubility of glucocorticoids, a fraction of the compounds is already dissolved in the aqueous supernatants of drug preparations (Bud>TCA>FP>MF>FF). The dissolution of FP, MF and FF was significantly enhanced in artificial nasal fluid and FF displayed the most pronounced enhancement of solubility in the presence of proteins. Consistent with this result, the highest retention in nasal tissue was observed for FF, followed by FP>MF>Bud>TCA. After washing of the nasal tissue samples, all compounds inhibited IL-8 release, with FF displaying the highest activity. CONCLUSION: FF displayed beneficial properties for nasal application. Its low application volume per spray is a prerequisite for effective drug utilization by avoiding immediate loss by nose runoff or drip down the throat. Sustained dissolution and high tissue binding of FF should contribute towards an extended presence of compounds in nasal tissue as a basis for a prolonged pharmacologic activity.
机译：背景：鼻内糖皮质激素是过敏性鼻炎的最有效药物治疗。到目前为止，尚无临床数据可将糠酸氟替卡松（FF）与其他鼻内应用的糖皮质激素进行比较。目的：由于药物的药代动力学行为决定着其在治疗靶位点的存在，因此我们比较了醋酸曲安奈德（TCA），布地奈德（Bud），丙酸氟替卡松（FP）和糠酸莫米松（MF）与FF的体外特性。另外，我们确定了洗净后存在于人鼻组织样品中的糖皮质激素部分的抗炎活性。方法：我们分析了该化合物在人造人鼻液中的溶解度，在人鼻组织中的滞留率以及市售药物制剂的典型喷雾量。作为一种抗炎措施，我们评估了对上皮细胞IL-8释放的抑制作用。结果：FF以每次喷雾的最小施用量提供。尽管糖皮质激素的水溶性低，但是一部分化合物已经溶解在药物制剂的水性上清液中（Bud> TCA> FP> MF> FF）。 FP，MF和FF在人造鼻液中的溶解度显着增强，FF在蛋白质存在下显示出最明显的溶解度增强。与此结果一致，FF在鼻组织中的保留最高，其次是FP> MF> Bud> TCA。清洗鼻腔组织样品后，所有化合物均抑制IL-8释放，其中FF表现出最高活性。结论：FF显示出对鼻应用有益的特性。每次喷洒时的低喷洒量是有效药物利用的先决条件，可避免因鼻涕或喉咙滴落而立即损失。 FF的持续溶解和高组织结合应有助于化合物在鼻组织中的持续存在，以此作为延长药理活性的基础。

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