Is the use of benzalkonium chloride as a preservative for nasal formulations a safety concern? A cautionary note based on compromised mucociliary transport
Is the use of benzalkonium chloride as a preservative for nasal formulations a safety concern? A cautionary note based on compromised mucociliary transport
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DOI：
10.1016/s0091-6749(00)90175-1
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发表时间：
2000-01-01
影响因子：
14.2
通讯作者：
Bernstein, IL
中科院分区：
文献类型：
--
作者：
Bernstein, IL
背景资料：局部鼻用溶液和混悬液给药系统可用于短效和长效血管收缩剂、异丙托铵、克罗埃宁、氮卓斯汀和糖皮质激素。鼻内糖皮质激素的使用已大大增加，因为这些药物的疗效已被证实用于治疗常年性和季节性变应性鼻炎。糖皮质激素鼻用制剂偶尔会引起烧灼、刺激和干燥等局部不良反应。苯扎氯铵（BKC）是一种季铵抗菌剂，包含在一些鼻用溶液中（包括糖皮质激素）以防止细菌生长，一些报告表明鼻喷雾剂中的BKC可能会引起不良反应，包括粘液纤毛运输减少、药物性鼻炎和中性粒细胞功能障碍。目的：本文通过检查BKC对以下粘膜纤毛运输特性的影响，总结了关于BKC作为鼻喷雾防腐剂可能产生的不良生物学效应的最新文献：纤毛运动，纤毛形式，纤毛节拍频率，电子显微镜，和粒子运动/糖精清除tests.Conclusion：动物和人类在体外的数据表明，BKC促进ciliostasis和减少mucociliary运输，可能部分掩盖了吸收和稀释作用发生在呼吸道粘液。这些可能的混杂因素可能导致几种不同的人体体内结果。应考虑使用不含BKC的糖皮质激素制剂，特别是主诉鼻灼热、干燥或刺激的患者。
Background: Topical nasal solution and suspension delivery systems are available for short- and long-acting vasoconstrictors, ipratropium, cromolyn, azelastine, and glucocorticosteroids. The use of intranasal glucocorticosteroids has increased substantially because the efficacy of these agents has been well established for the treatment of perennial and seasonal allergic rhinitis, Adverse local effects of burning, irritation, and dryness are occasionally associated with glucocorticosteroid nasal preparations. Benzalkonium chloride (BKC) is a quaternary ammonium antimicrobial agent included in some nasal solutions (including glucocorticosteroids) to prevent the growth of bacteria, Some reports suggest that BKC in nasal sprays may cause adverse effects, including reduced mucociliary transport, rhinitis medicamentosa, and neutrophil dysfunction.Objective: This article summarizes recent literature about possible adverse biologic effects associated with BKC as a nasal spray preservative by examining its effects on the following properties of mucociliary transport: ciliary motion, ciliary form, ciliary beat frequency, electron microscopy, and particle movement/saccharin clearance tests.Conclusion: Both animal and human in vitro data suggest that BKC promotes ciliostasis and reduction in mucociliary transport that may be partially masked by absorption and dilution effects occurring in respiratory mucus. These possible confounding factors may account for several disparate human in vivo results. The use of BKC-free glucocorticosteroid formulations should be considered, particularly in patients who complain of nasal burning, dryness, or irritation.