Inhalation

INH1021

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Some commercially available liquid nasal spray formulations include excipients that can act as penetration enhancers or mucoadhesives. They may thereby provide the benefit of increasing contact/residence time in the nasal cavity or increasing absorption of drug molecules by enhancing permeability through nasal mucosal membranes. This review may assist readers in considering the utility of various penetration enhancers and mucoadhesives for use in research and development. Inhalation OctOber 2021 11 Charles Shaw, PhD Renaissance Lakewood, LLC A review of nasal spray formulation excipients and their potential for enhancing drug delivery Penetration enhancers and mucoadhesives in liquid nasal spray formulations Introduction For many years, the nasal route of administration has been used very successfully for the non-invasive delivery of small molecule drugs. e anatomy and physiology of the nasal cavity have been exploited to deliver 1) locally acting medications, to combat ailments such as seasonal and year-round allergies, 2) systemically delivered drugs, via the highly vascu- larized turbinates (e.g., migraine treatments), and 3) drugs delivered directly to the central nervous sys- tem (nose-to-brain delivery), via the olfactory and trigeminal nerves (e.g., seizure treatments) [1]. Some commercially available liquid nasal spray formulations include excipients that can act as pene- tration enhancers or mucoadhesives, and may thereby provide the benefit of increasing contact/residence time in the nasal cavity or increasing absorption of drug molecules by enhancing permeability through nasal mucosal membranes. As liquid nasal sprays are now being developed to expand their use from traditional small molecule drug delivery systems to delivery of biologics and as a prophylaxis for respi- ratory diseases (including coronavirus treatments), the inclusion of penetration enhancers and muco- adhesives may become more important. is article, while not intended to be comprehensive, provides information that may assist readers in considering the utility of various penetration enhancers and mucoadhesives for use in research and development. Rationale for use of penetration enhancers and mucoadhesives e absorption of drugs through the biological membranes of the nasal cavity is influenced by the molecular weight, size and hydrophilicity/lipo- philicity of the drug, as well as the permeability of the membrane itself. Large molecular weight and water-soluble drugs (e.g., proteins and peptides) have relatively low membrane permeability [2]. is, together with the limited residence time within

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