Oral Drug Delivery Systems Utilizing Bile Salts
Summary
Oral drug delivery systems incorporating bile salts exploit the unique amphiphilic and solubilising properties of these endogenous molecules to enhance the bioavailability of poorly soluble or poorly permeable drugs. By forming mixed micelles, vesicles or bile salt–lipid complexes, these systems protect therapeutic agents from degradation in the gastrointestinal tract and facilitate transport across the mucosal barrier. Bile salts can promote drug solubilisation, modulate membrane fluidity and interact with transport proteins to improve uptake. Advances in nanoscale formulations—such as bilosomes, biloparticles and mixed micellar assemblies—have demonstrated increased stability in gastric and intestinal fluids, prolonged residence time at the absorption site and controlled release profiles. Such platforms accommodate a wide range of compounds, from small lipophilic molecules to complex biologics, and can be tailored with surface coatings or polymeric modifiers to target specific regions of the gut. Collectively, these approaches address fundamental obstacles in oral administration and hold considerable promise for transforming the delivery of next-generation pharmaceuticals on a global scale.
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Oral Drug Delivery Systems Utilizing Bile Salts publication trend
The graph below shows the total number of articles in oral drug delivery systems utilizing bile salts across all publications each year (not limited to Nature Index journals).
Technical terms
Bilosome: A vesicular carrier composed of phospholipids and bile salts, designed to resist bile-mediated degradation and enhance mucosal uptake.
Micelle: A spherical aggregate of amphiphilic molecules that solubilises lipophilic drugs in its hydrophobic core above the critical micelle concentration.
Critical micelle concentration (CMC): The minimum concentration of amphiphiles, such as bile salts, required to form micelles in aqueous solution.
Entrapment efficiency: The percentage of drug encapsulated within a carrier system relative to the total amount of drug used in formulation.
References
- ‘Poly phenolic phytoceutical loaded nano-bilosomes for enhanced caco-2 cell permeability and SARS-CoV 2 antiviral activity’: in-vitro and insilico studies. Drug Delivery (2023).
- Bilosomes and Biloparticles for the Delivery of Lipophilic Drugs: A Preliminary Study. Antioxidants (2023).
- Emerging Trends in Bilosomes as Therapeutic Drug Delivery Systems. Pharmaceutics (2024).
- Bile Acids and Their Derivatives as Potential Modifiers of Drug Release and Pharmacokinetic Profiles. Frontiers in Pharmacology (2018).
- Absorption-Enhancing Effects of Bile Salts. Molecules (2015).
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