Improvement of Intranasal Drug Delivery with Intravail(R) Alkylsaccharide Excipient as a Mucosal Absorption Enhancer Aiding in the Treatment of Conditions of the Central Nervous System

Intranasal drug administration is a commonly used route for therapeutic formulations, but there may be challenges associated with a lack of absorption and bioavailability, as well as damage to mucosal tissue. To address these issues, potential absorption enhancers that are generally nonirritating to nasal mucosal tissue have been investigated as excipients in intranasal formulations. Among those studied are alkylsaccharides, which are composed of sugars covalently coupled to at least one alkyl chain. Alkylsaccharides have been shown to be nontoxic and have been used in food products as emulsifiers. In clinical trials, alkylsaccharide excipients have demonstrated substantially increased absorption of therapeutic agents across mucosal membranes and have been shown to be applicable to a wide range of types of molecules and molecular weights. Because they are water and oil soluble, alkylsaccharide excipients can be used in formulations with both hydrophilic and hydrophobic drugs. They are also effective in safely stabilizing protein therapeutics. An example of an alkylsaccharide excipient is dodecyl maltoside (Intravail(R); 511 Da, stable long term when stored cold), which provides absorption enhancement by paracellular and transcellular routes. Dodecyl maltoside has been shown to be generally nonirritating to the nose and to promote systemic bioavailability. Dodecyl maltoside is used in US Food and Drug Administration-approved intranasal formulations of sumatriptan for migraine headaches and diazepam nasal spray for patients with epilepsy with acute seizure clusters. Plain Language Summary Nasal sprays can offer an easy and efficient route to deliver drugs. The nose can absorb drugs into the bloodstream quickly, and sprays require less patient training than injection or rectal treatments. However, the nasal cavity is small, and the spray must be concentrated and easily absorbed. Alkylsaccharides may enhance absorption in the nose. They have a good safety profile and are used in foods. Intravail (R) alkylsaccharides include dodecyl maltoside and tetradecyl maltoside. Nasal medications with dodecyl maltoside had drug concentrations and safety similar to injectable forms. Dodecyl maltoside is used in US Food and Drug Administration-approved nasal sprays for migraine (sumatriptan [Tosymra (R)]) and seizure clusters (diazepam [Valtoco (R)]). Dodecyl maltoside is also being tested in nasal sprays with other drugs that are absorbed too poorly or slowly on their own. With these new formulations, doctors and patients have more treatment choices and can select the best option.

Automated summary

Intranasal drug administration is a common route for therapeutic formulations, but challenges such as poor absorption and mucosal tissue damage exist. Potential absorption enhancers like alkylsaccharides have been investigated to address these issues, improving absorption of therapeutic agents across mucosal membranes and applicable to a wide range of molecules. Alkylsaccharide excipients, such as dodecyl maltoside, have shown to be nonirritating and effective in enhancing systemic bioavailability, and are used in FDA-approved intranasal formulations for migraine and epilepsy patients.