Medical Application of Synthetic Phospholipids as Liposomes and Drugs

Abstract

Synthetic phospholipids or analogues having well-defined purities are useful and stable carriers of drugs for a variety of medical therapies. Synthetic phospholipids possess the additional quality of being powerful drugs in the therapy of cancer and protozoaen diseases. In the last decade we have developed several different strategies for the large scale synthesis of phospholipids (50 to 100 kg). Here we describe methods involving the recombination of nonpolar and polar regions of phospholipid molecules which permit the creation of an unlimited variety of well-defined and characterizable phospholipids and of analogues. As an example for medical application we describe hexadecylphosphocholine (HePC) which in 1992 was approved and registered as a drug by the German Bundesgesundheitsamt. Recent studies have provided compelling evidence that erucylphosphocholine (ErPC) is an even more selective drug than HePC for systemic i.v. treatment of cancer.