Rationale utilization of phospholipid excipients: a distinctive tool for progressing state of the art in research of emerging drug carriers

Abstract

Phospholipids have a high degree of biocompatibility and are deemed ideal pharmaceutical excipients in the development of lipid-based drug delivery systems, because of their unique features (permeation, solubility enhancer, emulsion stabilizer, micelle forming agent, and the key excipients in solid dispersions) they can be used in a variety of pharmaceutical drug delivery systems, such as liposomes, phytosomes, solid lipid nanoparticles, etc. The primary usage of phospholipids in a colloidal pharmaceutical formulation is to enhance the drug's bioavailability with low aqueous solubility [i.e. Biopharmaceutical Classification System (BCS) Class II drugs], Membrane penetration (i.e. BCS Class III drugs), drug uptake and release enhancement or modification, protection of sensitive active pharmaceutical ingredients (APIs) from gastrointestinal degradation, a decrease of gastrointestinal adverse effects, and even masking of the bitter taste of orally delivered drugs are other uses. Phospholipid-based colloidal drug products can be tailored to address a wide variety of product requirements, including administration methods, cost, product stability, toxicity, and efficacy. Such formulations that are also a cost-effective method for developing medications for topical, oral, pulmonary, or parenteral administration. The originality of this review work is that we comprehensively evaluated the unique properties and special aspects of phospholipids and summarized how the individual phospholipids can be utilized in various types of lipid-based drug delivery systems, as well as listing newly marketed lipid-based products, patents, and continuing clinical trials of phospholipid-based therapeutic products. This review would be helpful for researchers responsible for formulation development and research into novel colloidal phospholipid-based drug delivery systems.

Keywords: Phospholipid based drug delivery; glycerophospholipids; lecithin; lipid excipients safety profile; lipid research; phasphatidylcholine; sphingophospholipids.