Synthetic Phospholipids as Excipients for Parenteral and Pulmonary Administration

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In pharmaceutical formulations, phospholipids obtained from plant or animal sources as well as synthetic phospholipids are used. Synthetic phospholipids possessing natural stereochemical configuration are preferably synthesized from sn-glycero-3-phosphocholine (GPC), using acylation and enzyme catalyzed reactions. The precursor GPC can be obtained from naturally occurring phospholipids.

In addition to natural phospholipids, synthetic phospholipids are becoming increasingly important in drug delivery, as can be seen from the number of drug products containing synthetic phospholipids. They mainly play a role in parenteral administration and inhalation dosage forms. Parenteral and inhalation products with synthetic phospholipids comprise liposomal formulations, lipid nanoparticles, diagnostic products, and dry powders for inhalation, respectively. Examples of intravenous products are provided in Table 1.

Synthetic phospholipids are used in parenteral depot formulations as well (Table 2).



Synthetic phospholipids can also be found in vaccines, in the form of lipid nano particles (LNPs) or liposomes in recently developed vaccine formulations for intramuscular administration for the delivery of messenger ribonucleic acid (mRNA) and a disease-related antigen, respectively. LNPs are also used for maintenance treatment of patients with chronic obstructive pulmonary disease intravenous administration of small interfering RNA (siRNA) in the treatment of rare diseases (Table 3).

Synthetic phospholipids in relevant inhalation products are listed in Table 4. Interestingly, the phospholipids are used in several types of formulations suitable for commonly used inhalation devices.




In the future, synthetic phospholipids and designer lipids may play a more important role in sophisticated drug delivery systems.

References

  1. van Hoogevest P, Luciani P. Recent Advances in the Use of Phospholipid Excipients in Local or Injectable Depot Formulations.
    Pharm. Ind. 2018, 8:1104.
  2. van Hoogevest P, Tiemessen H, Metselaar JM, Drescher S, Fahr A. The Use of Phospholipids to make Pharmaceutical Form Line Extensions. Eur. J. Lipid Sci. Technol. 2021, 2000297.

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