Synthetische Phospholipide als Hilfsstoffe zur parenteralen und pulmonalen Verabreichung
Übersichten
Key WordsSynthetische Phospholipide | Aminolipide | PEGylierte Lipide | Hilfsstoffe | Liposomen | Lipid-Nanopartikel
Abstract
Synthetic phospholipids as pharmaceutical excipients for parenteral and pulmonary administration
In pharmaceutical formulations phospholipids obtained from plant or animal sources as well as synthetic phospholipids are used. Synthetic phospholipids possessing the natural stereochemical configuration are preferably synthesized from sn-3-glycerophosphocholine (GPC) using acylation and enzyme catalyzed reactions. The precursor GPC can be obtained from naturally occurring phospholipids. In addition to natural phospholipids, synthetic phospholipids become more and more important in drug delivery, as can be seen from the number of drug products containing synthetic phospholipids. They play a role not only in parenteral administration but also in inhalation dosage forms. In parenteral and inhalation products, synthetic phospholipids are components of liposomal formulations, lipid nanoparticles and dry powders for inhalation, respectively. In the drug product Onpattro and COVID-19 vaccines synthetic phospholipids are used in combination with novel pH sensitive aminolipids and PEG-ylated lipids for parenteral delivery of RNA.
Korrespondenz:
Dr. Peter Hölig, Lipoid GmbH, Frigenstr. 4, 67065 Ludwigshafen (Germany), E-Mail: p.hoelig@lipoid.com
Zusammenfassung
In pharmazeutischen Formulierungen werden oft aus pflanzlichen oder tierischen Quellen gewonnene Phospholipide aber auch synthetische Phospholipide eingesetzt. Synthetische Phospholipide, die die natürliche stereochemische Konfiguration besitzen, werden vorzugsweise aus sn-Glycero-3-phosphocholin durch Acylierung und enzymkatalysierte Reaktionen synthetisiert. GPC als Startmaterial kann aus natürlich vorkommenden Phospholipiden gewonnen werden. Neben den natürlichen Phospholipiden
