Absorption Enhancing Excipients in Systemic Nasal Drug Delivery

Abstract

Intranasal drug delivery is becoming an increasingly important form of drug administration for chronic and chronic-intermittent diseases. Important new applications in development include drugs for diabetes, osteoporosis, obesity, certain types of convulsive disorders, migraine headaches, symptomatic pain relief, nausea, and anxiety, among others. Transmucosal absorption across the nasal mucosa is generally limited to molecules under 1,000 Da in size. Systemic delivery of molecules larger than this requires formulation with a suitable transmucosal absorption enhancer. More than one hundred potential transmucosal absorption enhancing excipients have been tested to date.  Nearly all have failed to be practical due to poor effectiveness or unacceptable toxicity to mucosal tissue. Alkylsaccharides, cyclodextrins, and chitosan's have emerged as the leading candidates for potential broad clinical applications and are allowing development of convenient, patient-friendly, needle free formulations of small molecule drugs, as well as peptide and protein drugs that can be administered at home, at work, or in other public and private settings outside of the doctor’s office or hospital environment.