Opportunity and challenges of nasal powders: Drug formulation and delivery

• Published in: European journal of pharmaceutical sciences Vol. 113; pp. 2 - 17
• Main Authors: Tiozzo Fasiolo, Laura, Manniello, Michele Dario, Tratta, Elena, Buttini, Francesca, Rossi, Alessandra, Sonvico, Fabio, Bortolotti, Fabrizio, Russo, Paola, Colombo, Gaia
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 15.02.2018
• Subjects: Administration, Intranasal; Animals; Beclomethasone - pharmacology; Biological Availability; Budesonide - pharmacology; Chemistry, Pharmaceutical - methods; Device; Dexamethasone - analogs & derivatives; Dexamethasone - pharmacology; Drug Carriers - chemistry; Drug Liberation; Equipment and Supplies; Excipients - chemistry; Humans; Microparticle; Mucous Membrane - metabolism; Nasal Absorption; Nasal drug delivery; Nose-to-brain; Particle engineering; Permeability; Powder; Powders - chemistry; Rhinitis - drug therapy; Solubility; Water - chemistry; Nasal drug delivery; BCS; MRI; NSAID; Device; Particle engineering; Microparticle; API; GRAS; Nose-to-brain; Powder; AUC
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2017.09.027

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. [Display omitted]