TABLE 2.
Characteristics of absorption‐enhancing agents suitable for intranasal administration 39
| Absorption enhancer | Concentration | Mean fold increase in brain delivery a | Variability of mean fold increase, range | Nasal mucosal toxicity |
|---|---|---|---|---|
| Chitosan | .5% wt/vol | 6.1 | 3–11 fold | No |
| Decyl maltoside | .5% wt/vol | 4.3 | ND | No |
| n‐Dodecyl beta‐D‐maltoside (Intravail A3) | .25% wt/vol | 7.6 | 6–9 fold | No |
| Propylene glycol | 10%–20% | 4.5 | 4–10 fold | No |
| Heptakis‐(3‐O‐methyl‐2,6‐di‐O‐pentyl)‐β‐cyclodextrin | 5% wt/vol | 3.1 | ND | Yes |
| 1,2 Didecanoyl‐glycero‐3‐phosphocholine | 2% wt/vol (as oil emulsion) | 9.6 | ND | Yes |
| Glycocholate | 1% wt/vol | 17.6 | ND | Yes |
| Taurocholate | 1% wt/vol | 14 | ND | Yes |
| Tauroursodeoxycholate | 1% wt/vol | 4 | ND | Yes |
Source: US Patent No. 8883728 B2: Intranasal Administration of Active Agents to the Central Nervous System.
Abbreviations: ND, not done; wt/vol, weight/volume concentration.
a
Represents mean fold increase in brain delivery efficiency of nasally administered Homo sapiens‐derived antibody Fc (hFc) fragment relative to control formulation (phosphate‐buffered saline; pH 7.4 and 36 mg/ml hFc).