Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

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The use of CDs in nasal formulations allowed obtaining versatile drug delivery systems intended for local and systemic effects, as well as for nose-to-brain transport of drugs. In vitro and in vivo models currently
employed are suitable to analyze the effects of CDs in nasal formulations.

The drugs permeating across the respiratory mucosa can easily reach the bloodstream, whereas those permeating the olfactory mucosa can directly target the cerebrospinal fluid (CSF). Data suggest that
CDs may have different aptitudes in promoting the drug permeation across the respiratory (poor in neuron-like components) or olfactory (rich in neuron-like components) mucosa, HP-B -CD or RM-B -CD (<10%) solution did not appear toxic for nasal mucosa.

Two drugs already marketed:

BaqsimiTM (Eli Lilly, Indianapolis, IN, USA) is a nasal dry powder formulation containing betadex as a permeation enhancer for glucagon, used to treat severe hypoglycemia in patients with diabetes.

Aerodiol® (Servier, Suresnes, France) is a nasal spray solution of 17 -estradiol hemihydrate containing randomly methylated betadex used for hormone replacement therapy.

The review gives several examples on various in vitro and in vivo models for studying the systemic effects of CDs on nasal administration of drugs as well as the use of nasally administrated CDs as actives e.g. in Alzheimer disease.

Rassu, G.; Sorrenti, M.; Catenacci, L.; Pavan, B.; Ferraro, L.; Gavini, E.; Bonferoni, M.C.; Giunchedi, P.; Dalpiaz, A. Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives? Pharmaceutics 2021, 13, 1180.

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