Effective incorporation of insulin in mucus permeating self-nanoemulsifying drug delivery systems
| Autor: | Vassilis Bourganis, Konstantina Karidi, Olga Kammona, Costas Kiparissides, Katerina Kontonikola, Theodora Karamanidou |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Swine
Chemistry Pharmaceutical medicine.medical_treatment Administration Oral Pharmaceutical Science Permeability Phase Transition Surface-Active Agents chemistry.chemical_compound Drug Delivery Systems Pulmonary surfactant medicine Animals Insulin Particle Size Phosphatidylglycerol Drug Carriers Chromatography Phosphatidylglycerols General Medicine Trypsin Mucus Drug Liberation chemistry Ionic strength Permeability (electromagnetism) Drug delivery Nanoparticles Emulsions Biotechnology medicine.drug |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 97:223-229 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2015.04.013 |
| Popis: | The development of a novel, mucus permeating SNEDDS formulation for oral insulin delivery containing a hydrophobic ion pair of insulin/dimyristoyl phosphatidylglycerol (INS/DMPG) is presented. Three oil/surfactant/cosurfactant combinations and 27 weight ratios of oil, surfactant and cosurfactant for each combination were evaluated with the aid of ternary phase diagrams, for the incorporation of the protein/phospholipid complex. The developed formulation was characterized by an average droplet diameter of 30-45 nm. Depending on the initial protein concentration, the loading of insulin in SNEDDS varied between 0.27 and 1.13 wt%. The therapeutic protein was found to be efficiently protected from enzymatic degradation by intestinal enzymes (i.e., trypsin, α-chymotrypsin). The SNEDDS formulation exhibited increased mucus permeability and did not appear to be affected by ionic strength. The incorporation of INS/DMPG in SNEDDS prevented an initial burst release of insulin. INS/DMPG loaded SNEDDS were found to be non-cytotoxic up to a concentration of 2mg/ml. According to the reported results, the incorporation of the hydrophobic ion pair of INS/DMPG in SNEDDS could be regarded as a promising strategy for the oral delivery of insulin. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect