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Formulation and administration parameters for the optimisation of nasal deposition pattern of sprayable in situ gelling fluticasone delivery system

Nasal delivery receives much attention as an attractive route of drug administration. The anatomy and physiology of the nasal cavity are recognized as the most critical factors in drug delivery system design, especially mucociliary clearance that limits drug-to-mucosal surface contact time [1]. However, the crucial parameter for the treatment outcome is drug deposition within the nasal cavity [2]. The purpose of this study is to set the basis for the development of sprayable in situ gelling fluticasone delivery system and to recognize the formulation and administration parameters with the highest impact on nasal deposition pattern. Pectin based in situ gelling fluticasone suspensions have been prepared using Tween 80 as a suspending agent and mannitol as a tonicity agent. Sodium hyaluronate was evaluated as potential gel-structuring and bioactive formulation constituent. In situ gelling systems were characterised in terms of suspended particle size (Olympus BH-2 microscope, Japan), rheological properties (Rheometer MCR 102, Anton Paar, Austria), sprayability/droplet size distribution (Malvern Spraytec, UK) and nasal deposition pattern (human nasal cavity model, Koken. Co. Ltd., Japan). Pectin based in situ gelling fluticasone suspensions have been successfully prepared. Under formulation and administration parameters employed, appropriate window of droplet size distribution and spray angle was reached resulting in targeted deposition pattern within the nasal cavity. Screening studies revealed the parameters to be included in experimental design aiming to elucidate their relation with in situ gelling system properties/deposition pattern. Such an approach potentiates the development of fluticasone in situ gelling system with built-in quality attributes in a cost and time-saving manner. This work has been supported in part by Croatian Science Foundation under the project UIP-2017- 05-4592. REFERENCES 1. Karavasili C. et al. Drug Descov. Today 21, 157-166 (2016) 2. Xi J. et al. Pharm. Res. 33, 1527-1541 (2016)

Fluticasone ; Pectin ; Gellan gum ; Sodium hyaluronate ; In situ gelling ; Nasal deposition

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