Verhoging van de biologische beschikbaarheid: verbetering van de permeabiliteit van geneesmiddelen

After an oral administration, drug absorption through the intestinal epithelium is rate-limited due to poor permeability. Various approaches can enhance drug permeability.

One approach is the design of lipid-based formulations with enhanced dissolution and solubility. These target physiological mechanisms such as bile salt secretion stimulation, gastric emptying rate reduction, decreased luminal degradation, and enhanced lymphatic system uptake.

Lipid-based formulations are available as lipid solutions, suspensions, microemulsions, nanoparticles, and liposomes.

These systems have low aqueous solubility, sustained release, and reduced toxicity.

Another method is the ion pairing approach, which involves the co-administration of hydrophilic drugs with suitable lipophilic counterions. This increases the oral bioavailability of drugs like atenolol.

The third approach is the use of penetration enhancers along with hydrophilic drugs. The lipid part of the penetration enhancers interacts with the polar components of membrane phospholipids to facilitate the transport of drugs across the biomembrane. Examples include EDTA, oleic acid, and salicylate.