Improvement of Intranasal Drug Delivery with Intravail® Alkylsaccharide Excipient as a Mucosal Absorption Enhancer Aiding in the Treatment of Conditions of the Central Nervous System.
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| Abstract |
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®; 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.
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| Authors | Adrian L Rabinowicz, Enrique Carrazana, Edward T Maggio |
| Journal | Drugs in R&D (Drugs R D) Vol. 21 Issue 4 Pg. 361-369 (Dec 2021) ISSN: 1179-6901 [Electronic] New Zealand |
| PMID | 34435339 (Publication Type: Journal Article, Review) |
| Copyright | © 2021. The Author(s). |
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