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Abstract
Lactoferrin (Lf), a bioactive protein initially found in many biological secretions including milk, is regarded as the nutritional supplement or therapeutic ligand due to its multiple functions. Research on its mode of action reveals that intact Lf or its active peptide (i.e., lactoferricin) shows an important multifunctional performance. Oral delivery is considered as the most convenient administration route for this bioactive protein. Unfortunately, Lf is sensitive to the gastrointestinal (GI) physicochemical stresses and lactoferricin is undetectable in GI digesta. This review introduces the functionality of Lf at the molecular level and its degradation behavior in GI tract is discussed in detail. Subsequently, the absorption and transport of Lf from intestine into the blood circulation, which is pivotal to its health promoting effects in various tissues, and some assisting labeling methods are discussed. Stabilization technologies aiming at preserving the structural integrity and functional properties of orally administrated Lf are summarized and compared. Altogether, this work comprehensively reviews the structure-function relationship of Lf, its oral fate and the development of stabilization technologies for the enhancement of the oral bioavailability of Lf. The existing limitations and scope for future research are also discussed.