Self-Emulsifying Drug Delivery Systems for Oral Biopharmaceuticals

Summary

Self‐emulsifying drug delivery systems (SEDDS) represent a class of lipid‐based nanocarriers designed to overcome the inherent challenges of administering peptides, proteins and other biopharmaceuticals by mouth. By combining selected oils, surfactants and co-solvents into isotropic pre-concentrates, SEDDS form fine oil-in-water emulsions upon mild agitation in gastrointestinal fluids. This process enhances the apparent solubility of hydrophobic macromolecules, shields them from proteolytic degradation and facilitates transport across the mucus barrier and intestinal epithelium. Variants such as self-nanoemulsifying drug delivery systems (SNEDDS) produce droplets in the sub-100 nm range, further improving mucosal permeation and lymphatic uptake. Innovations in hydrophobic ion pairing, reverse micelle incorporation and solidification strategies have elevated payload capacity, stability and dosage flexibility—enabling conversion into powders or tablets without loss of biological activity. Quality by Design approaches ensure consistent droplet size distribution, zeta potential control and reproducible in vitro‐in vivo performance. Collectively, these advances underscore the global potential of SEDDS to transform oral delivery of therapeutic peptides and proteins, reduce dependence on injections and expand access to biopharmaceutical treatments.

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Self-Emulsifying Drug Delivery Systems for Oral Biopharmaceuticals publication trend

The graph below shows the total number of articles in self-emulsifying drug delivery systems for oral biopharmaceuticals across all publications each year (not limited to Nature Index journals).

Technical terms

Self-emulsifying drug delivery system (SEDDS): An isotropic mixture of oils, surfactants and co-solvents that spontaneously forms fine oil-in-water emulsions in the gastrointestinal tract, enhancing solubility and absorption of lipophilic drugs and biopharmaceuticals.

Self-nanoemulsifying drug delivery system (SNEDDS): A subtype of SEDDS designed to produce nanoscale droplets (typically <100 nm) for improved mucosal permeation and lymphatic transport.

Hydrophobic ion pairing: A formulation technique that complexes water-soluble peptides or proteins with lipophilic counterions to increase their incorporation into lipid-based carriers and protect against enzymatic degradation.

Reverse micelle: A nanostructure formed by surfactants in a non-polar phase that encloses aqueous regions, enabling encapsulation and controlled release of hydrophilic biomolecules within SEDDS.

Zeta potential: The electrical potential at the slipping plane of colloidal droplets, which influences emulsion stability and interactions with mucosal surfaces.

References

  1. Self‐Emulsifying Drug Delivery Systems (SEDDS) Containing Reverse Micelles: Advanced Oral Formulations for Therapeutic Peptides. Advanced Healthcare Materials (2023).
  2. Quality by Design-Based Development of Solid Self-Emulsifying Drug Delivery System (SEDDS) as a Potential Carrier for Oral Delivery of Lysozyme. Pharmaceutics (2023).
  3. Oral delivery of therapeutic peptides and proteins: Technology landscape of lipid-based nanocarriers. Advanced Drug Delivery Reviews (2022).
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