Injectable formulations represent one of the most extensive application areas for phospholipids, with fat emulsions, liposomes, and lipid nanoparticles (LNPs) being the most representative. In fat emulsions, phospholipids—such as egg yolk lecithin—serve as emulsifiers, stabilizing the oil–water interface and dispersing poorly soluble, lipophilic drugs into nano-sized emulsion droplets, thereby preventing drug precipitation while enhancing the formulation’s biocompatibility for intravenous administration. Liposomes utilize a phospholipid bilayer as their capsule wall, enabling simultaneous encapsulation of both hydrophilic and lipophilic drugs, mimicking biological membrane structures to achieve targeted drug delivery and reduce systemic toxic side effects. They are now widely employed in delivering anti-tumor and anti-infective agents, with numerous clinically approved products [1,2]. In LNPs, phospholipids work synergistically with cholesterol to form nano-scale delivery vehicles capable of efficiently encapsulating nucleic acid drugs such as mRNA, protecting them from enzymatic degradation and promoting intracellular delivery; they are among the core excipients of mRNA vaccines [3].

In pulmonary inhalation formulations, phospholipids play a crucial role thanks to their unique interfacial activity. The lung mucosal surface is rich in lipids, and phospholipids can lower the formulation’s surface tension, improving the dispersion of aerosolized particles and their deposition rate in the lungs, enhancing drug–mucosa compatibility, and facilitating transmucosal absorption. At the same time, phospholipids improve drug solubility, reduce drug retention and loss in the respiratory tract, and increase local drug concentrations in the lungs, making them suitable for the topical treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease [4].

In topical formulations, the multifunctionality of phospholipids is fully demonstrated. As penetration enhancers, unsaturated phospholipids can “soften” or “fluidize” the skin’s stratum corneum, helping drugs penetrate the skin barrier and boosting local drug concentrations; saturated phospholipids, on the other hand, prolong the residence time of drugs on the skin surface, extending their therapeutic effect. Additionally, phospholipids serve as emulsifiers and moisturizers, improving the texture of creams, gels, and other topical dosage forms, enhancing skin tolerability—particularly beneficial for sensitive skin when used in topical medications and transdermal delivery systems, such as those for anti-inflammatory or whitening agents—and they can also aid in improving skin condition by repairing damaged cell membranes [5].

Guangzhou Baiyunshan Hanfang Modern Pharmaceutical Co., Ltd. boasts advanced phospholipid production lines and a comprehensive quality management system, offering a wide range of functional phospholipid excipients to support the development and collaboration on various pharmaceutical products!

Injectable formulations represent one of the most extensive application areas for phospholipids, with fat emulsions, liposomes, and lipid nanoparticles (LNPs) being the most representative. In fat emulsions, phospholipids—such as egg yolk lecithin—serve as emulsifiers, stabilizing the oil–water interface and dispersing poorly soluble, lipophilic drugs into nano-sized emulsion droplets, thereby preventing drug precipitation while enhancing the formulation’s biocompatibility for intravenous administration. Liposomes utilize a phospholipid bilayer as their capsule wall, enabling simultaneous encapsulation of both hydrophilic and lipophilic drugs, mimicking biological membrane structures to achieve targeted drug delivery and reduce systemic toxic side effects. They are now widely employed in delivering anti-tumor and anti-infective agents, with numerous clinically approved products [1,2]. In LNPs, phospholipids work synergistically with cholesterol to form nano-scale delivery vehicles capable of efficiently encapsulating nucleic acid drugs such as mRNA, protecting them from enzymatic degradation and promoting intracellular delivery; they are among the core excipients of mRNA vaccines [3].

In pulmonary inhalation formulations, phospholipids play a crucial role thanks to their unique interfacial activity. The lung mucosal surface is rich in lipids, and phospholipids can lower the formulation’s surface tension, improving the dispersion of aerosolized particles and their deposition rate in the lungs, enhancing drug–mucosa compatibility, and facilitating transmucosal absorption. At the same time, phospholipids improve drug solubility, reduce drug retention and loss in the respiratory tract, and increase local drug concentrations in the lungs, making them suitable for the topical treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease [4].

In topical formulations, the multifunctionality of phospholipids is fully demonstrated. As penetration enhancers, unsaturated phospholipids can “soften” or “fluidize” the skin’s stratum corneum, helping drugs penetrate the skin barrier and boosting local drug concentrations; saturated phospholipids, on the other hand, prolong the residence time of drugs on the skin surface, extending their therapeutic effect. Additionally, phospholipids serve as emulsifiers and moisturizers, improving the texture of creams, gels, and other topical dosage forms, enhancing skin tolerability—particularly beneficial for sensitive skin when used in topical medications and transdermal delivery systems, such as those for anti-inflammatory or whitening agents—and they can also aid in improving skin condition by repairing damaged cell membranes [5].

Guangzhou Baiyunshan Hanfang Modern Pharmaceutical Co., Ltd. boasts advanced phospholipid production lines and a comprehensive quality management system, offering a wide range of functional phospholipid excipients to support the development and collaboration on various pharmaceutical products!

References

[1] Lipid-Based Drug Delivery Systems for Disease Management[J]. PMC, 2025.

[2] Reem M. Senjab, et al. Advances in Liposomal Nanotechnology: From Concept to Clinics[J]. RSC Publishing, 2026.

[3] Neill J. Lip Trott, et al. Redefining LNP Composition: Phospholipid and Sterol-Driven Modulation of mRNA Expression and Immune Outcomes[J]. RSC Publishing, 2025.

[4] Elucidating the Structure of Endogenous Phospholipids in the In Vivo Absorption of Octreotide Following Lung Administration[J]. PubMed, 2025.

[5] Synergistic Penetration Enhancement Effect of Ethanol and Phospholipids on the Topical Delivery of Cyclosporin A[J]. PubMed, 2025.