Lipid-Based Drug Delivery Systems for Enhanced Bioavailability

Summary

Lipid-based drug delivery systems encompass a range of formulations in which therapeutic agents are incorporated into or associated with lipid components to improve solubility, stability and absorption. By leveraging the natural affinity of lipids for biological membranes, these systems protect labile drugs from degradation in the gastrointestinal tract, facilitate transport across epithelial barriers and promote uptake into the lymphatic system, thereby bypassing hepatic first-pass metabolism. Common platforms include vesicular carriers such as liposomes, dispersed lipid droplets in self-emulsifying and self-nanoemulsifying systems, solid lipid nanoparticles and nanostructured lipid carriers. Each class offers distinct advantages: liposomes enable encapsulation of both hydrophilic and lipophilic compounds within bilayer structures; self-nanoemulsifying formulations produce fine oil-in-water emulsions in situ to enhance dissolution of poorly water-soluble drugs; and solid lipid matrices afford controlled release and improved physical stability. Collectively, these approaches address global challenges in oral drug administration, support the development of novel therapeutics and repurposed agents, and underpin the success of emerging modalities such as nucleic acid vaccines and targeted oncology treatments.

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Lipid-Based Drug Delivery Systems for Enhanced Bioavailability publication trend

The graph below shows the total number of articles in lipid-based drug delivery systems for enhanced bioavailability across all publications each year (not limited to Nature Index journals).

Technical terms

Liposome: A colloidal carrier composed of one or more phospholipid bilayers enclosing an aqueous core, capable of encapsulating hydrophilic and lipophilic drugs and enhancing stability and targeted delivery.

Self-nanoemulsifying drug delivery system (SNEDDS): An isotropic mixture of oils, surfactants and co-solvents that spontaneously forms a fine oil-in-water nanoemulsion upon dilution in gastrointestinal fluids, improving solubilisation of lipophilic drugs.

Bioavailability: The fraction of an administered dose of unchanged drug that reaches the systemic circulation and becomes available for therapeutic action.

Lymphatic transport: The absorption pathway by which lipophilic drug-loaded lipid particles enter intestinal lymphatic vessels, thereby bypassing first-pass hepatic metabolism and enhancing systemic exposure.

References

  1. A Review of Liposomes as a Drug Delivery System: Current Status of Approved Products, Regulatory Environments, and Future Perspectives. Molecules (2022).
  2. Methods of Liposomes Preparation: Formation and Control Factors of Versatile Nanocarriers for Biomedical and Nanomedicine Application. Pharmaceutics (2022).
  3. Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches. Pharmaceutics (2020).
  4. Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment. Frontiers in Pharmacology (2019).
  5. Development of Solid SEDDS, V: Compaction and Drug Release Properties of Tablets Prepared by Adsorbing Lipid-Based Formulations onto Neusilin® US2. Pharmaceutical Research (2013).
  6. Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery. Pharmaceutics (2020).

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