Work

The impact of formulation design on the oral bioavailability of omega-3 polyunsaturated fatty acids

Year: 2025

Type: review

Abstract: Omega-3 polyunsaturated fatty acids (n-3 PUFA) are essential dietary supplements with widespread health benefits. However, achieving therapeutic n-3 PUFA levels in systemic circulation represents a significant dosing challenge, complicated by a complex interaction between different physiological and chemical factors. Recently, significant efforts have been directed towards creating “bio-accessible” n-3 PUFA formulations that overcome this dosing challenge by enabling increased oral absorption across the small intestine. However, the impact of varying physiochemical formulation properties on n-3 PUFA bioavailability remains poorly understood and requires further investigation. This review explores the impact of formulation design, including self-emulsifying systems, micro- and nano-emulsions, chewable gels, and microencapsulation, on n-3 PUFA pharmacokinetics, considering both clinical and preclinical investigations. Key challenges in developing highly bioavailable n-3 PUFA formulations and quantifying their absorption, biodistribution and metabolism are discussed. Finally, recent progress in developing next-generation n-3 PUFA formulations, including solid lipid nanoparticles and nanostructured lipid carriers, and their targeting through innovative lipid structuring approaches will be addressed. The oral bioavailability of n-3 PUFA is ultimately influenced by multiple design factors related to each formulation strategy, underscoring the need for a systematic formulation approach that involves comprehensive testing of candidate formulation under simulated gastrointestinal conditions. • PUFA pharmacokinetics is controlled by lipid digestion kinetics in the GI tract. • Enabling high absorption of PUFA presents a significant formulation challenge. • Colloidal and interfacial formulations properties dictate PUFA pharmacokinetics. • SEDDS emerge as standout PUFA formulation strategy for enhancing pharmacokinetics. • Improved in vitro & in vivo models are needed for predicting PUFA pharmacokinetics.

Source: Food Research International

DOI: 10.1016/j.foodres.2025.116171

Authors: Amer Abdelhafez, Zahra Khabir, Clive A. Prestidge, Alfonso Garcia-Bennett, Paul Joyce

Institutions: University of South Australia, Macquarie University

Language: English

Topic: Drug Solubulity and Delivery Systems

Subfield: Pharmaceutical Science

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,320