Absorption of polyethylene glycol (PEG) polymers: the effect of PEG size on permeability
| Autor: | Juergen W. Pfeiffer, Jennifer Riggs-Sauthier, Hema Gursahani, David Lechuga-Ballesteros, C. Simone Fishburn |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Male
Polymers Pharmaceutical Science Polyethylene glycol Respiratory Mucosa Permeability Absorption Polyethylene Glycols Rats Sprague-Dawley chemistry.chemical_compound Polymer chemistry PEG ratio Animals Particle Size chemistry.chemical_classification Dose-Response Relationship Drug technology industry and agriculture Polymer Rats Membrane chemistry Permeability (electromagnetism) PEGylation Biophysics Particle size Absorption (chemistry) |
| Zdroj: | Journal of pharmaceutical sciences. 98(8) |
| ISSN: | 1520-6017 |
| Popis: | Polyethylene glycol (PEG) polymers are large amphiphilic molecules that are highly hydrated in solution. To explore the permeability properties of different sized PEG polymers across epithelial membranes in vivo, we examined the absorption of fluorescently labeled PEG conjugates sized 0.55-20 kDa from the lung, since this system provides a reservoir that limits rapid diffusion of molecules away from the site of delivery and enables permeability over longer times to be examined. Following intratracheal delivery in rats, the PEG polymers underwent absorption with first-order kinetics described by single exponential decay curves. PEG size produced a marked influence on the rate of uptake from the lung, with half-lives ranging from 2.4 to 13 h, although above a size of 5 kDa, no further change in rate was observed. PEG size likewise affected retention in alveolar macrophages and in lung tissue; whereas smaller PEG sizes (2 kDa) were effectively cleared within 48 h, larger PEG sizes (5 kDa) remained in lung cells and tissue for up to 7 days. These data demonstrate that PEG polymers can be absorbed across epithelial membranes and that PEG size plays a dominant role in controlling the rate and mechanism of absorption. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text