Food and Drug Department, University of Parma, Viale delle Scienze 27A, 43124 Parma, Italy; Department of Life Sciences and Biotechnology, University of Ferrara, Via Fossato di Mortara 17/19, 44121 Ferrara, Italy.
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano (SA), Italy.
Eur J Pharm Sci. 2018 Feb 15;113:2-17. doi: 10.1016/j.ejps.2017.09.027. Epub 2017 Sep 20.
In the field of nasal drug delivery, among the preparations defined by the European Pharmacopoeia, nasal powders facilitate the formulation of poorly water-soluble active compounds. They often display a simple composition in excipients (if any), allow for the administration of larger drug doses and enhance drug diffusion and absorption across the mucosa, improving bioavailability compared to nasal liquids. Despite the positive features, however, nasal products in this form still struggle to enter the market: the few available on the market are Onzetra Xsail® (sumatriptan) for migraine relief and, for the treatment of rhinitis, Rhinocort® Turbuhaler® (budesonide), Teijin Rhinocort® (beclomethasone dipropionate) and Erizas® (dexamethasone cipecilate). Hence, this review tries to understand why nasal powder formulations are still less common than liquid ones by analyzing whether this depends on the lack of (i) real evidence of superior therapeutic benefit of powders, (ii) therapeutic and/or commercial interest, (iii) efficient manufacturing methods or (iv) availability of suitable and affordable delivery devices. To this purpose, the reader's attention will be guided through nasal powder formulation strategies and manufacturing techniques, eventually giving up-to-date evidences of therapeutic efficacy in vivo. Advancements in the technology of insufflation devices will also be provided as nasal drug products are typical drug-device combinations.
在鼻腔给药领域，在欧洲药典定义的制剂中，鼻腔粉末制剂有利于将水溶性差的活性化合物制成制剂。它们通常在辅料（如果有）中具有简单的组成，允许给予更大剂量的药物，并增强药物在黏膜中的扩散和吸收，与鼻腔液体相比提高生物利用度。然而，尽管具有这些积极特点，但这种形式的鼻腔产品仍难以进入市场：市场上仅有少数几种产品，用于缓解偏头痛的 Onzetra Xsail®（舒马曲坦）和用于治疗鼻炎的 Rhinocort® Turbuhaler®（布地奈德）、Teijin Rhinocort®（丙酸倍氯米松）和 Erizas®（地塞米松西替卡因）。因此，本文试图通过分析鼻腔粉末制剂是否由于以下原因（i）缺乏粉末治疗优势的真正证据，（ii）治疗和/或商业利益，（iii）有效的制造方法或（iv）合适且负担得起的给药装置的缺乏而仍然不如液体制剂常见，来了解为什么鼻腔粉末制剂仍然不如液体制剂常见。为此，将引导读者关注鼻腔粉末制剂的策略和制造技术，最终提供体内治疗效果的最新证据。作为鼻腔药物产品的典型药物-器械组合，还将提供吸入装置技术的进步。
