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Human Clinical Nasal Deposition and Retention from Nonaqueous and Aqueous Steroid Inhalers

Leach CL, Chand R, Kuehl PJ.

Respiratory Drug Delivery 2016. Volume 1, 2016: 193-202.

Abstract:

The nasal deposition of commonly used drug products such as aqueous formulations and propellant based formulations is described in rhinitis patients. This study quantified the regional nasal deposition of an HFA-beclomethasone nasal spray, a fluticasone propionate nasal spray, and a mometasone furoate monohydrate nasal spray in rhinitis patients. This was an open label, crossover study in nine patients with allergic rhinitis. The regional nasal deposition of the three nasal products was assessed following the delivery of the 99mTc-radiolabeled drug in each respective product. The resultant gamma images were merged with magnetic resonance images to quantify regional deposition within the patients’ noses. The HFA-beclomethasone propellant based formulation showed an increased retention of drug in the nasal cavity compared with the two aqueous formulations (i.e., fluticasone and mometasone) over time. The aqueous-based products showed an increased amount of the delivered dose that dripped from the patient’s nostrils (e.g., 6/8 patients for each of the aqueous formulations and 0/8 patients for the HFA propellant formulation). The percentage of delivered dose that deposited in the back of the throats of the patients was increased and variable (e.g., 0.1% to 17.6% with fluticasone and 0.0 to 4.7% for mometasone) for the aqueous formulations compared to dose delivered for the HFA propellant formulation (e.g., 0.0% to 1.7% for HFA-beclomethasone). The regional deposition of the HFA propellant-based formulation resulted in increased retention of beclomethasone in the nasal cavity and decreased deposition in the back of the throat compared to the two aqueous formulations. A separate clinical pharmacokinetic study showed that HFA-beclomethasone nasally administered had substantially lower systemic bioavailability than an orally inhaled HFA-beclomethasone product. Additionally nasal HFA-beclomethasone showed no significant effect on systemic HPA-axis function.