Gastric Digestion of Bovine Lactoferrin In Vivo in Adults

Abstract

Lactoferrin (LF), an iron-binding glycoprotein present in milk and other endocrine and exocrine secretions, may exert a number of physiologic effects in the intestines. To study the effects of oral LF supplementation in vivo in the gastrointestinal tract, information about the gastric survival of LF in vivo is important. We tested 12 healthy volunteers (age 21 +/- 0.3 y) on 3 separate d according to a randomized, cross-over design. A test drink containing 4.5 g of bovine LF (20% iron-saturated LF; apoLF) in the presence of a gastric pH buffer (0.1 mol/L sodium citrate/citric acid; apoLFbuf), apoLF without the buffer (apoLF) or iron-saturated LF (holoLF) was administered into the stomach using nasogastric intubation. Gastric emptying rate, determined by a marker dilution technique, did not differ among any of these drinks. Gastric survival of LF, analyzed by gel permeation chromatography under denaturing conditions, was 64%, 62% and 79% after consumption of the apoLFbuf, apoLF and holoLF test drinks, respectively. Addition of the gastric pH buffer initially lowered intragastric pH because of its hydroxide buffering effect. However, it did not elevate intragastric pH over a prolonged period and thereby inhibit intragastric LF breakdown. We conclude that after oral administration, substantial amounts of apoLF and holoLF survive gastric transit.

Recombinant human lactoferrin ingestion attenuates indomethacin-induced enteropathy in vivo in healthy volunteers

“…This implies that at least 76% of the indomethacin was present as free indomethacin after 22 min. In previous studies, we showed that after 7 min almost half of the test drink ingested is emptied from the stomach, while after 22 min most if not all of the test drink is emptied from the stomach into the small intestine (Troost et al, 2001). Hence, in the present study, indomethacin entered the small intestine predominantly unbound to LF.…”

“…The observed protective effect of oral LF administration can probably not be explained by LF-indomethacin binding. We previously showed that the major part of orally ingested LF survives gastric passage in vivo in adults, leaving most of the LF intact until it enters the intestine (Troost et al 2001).…”

Inhibitory effects of orally administrated liposomal bovine lactoferrin on the LPS-induced osteoclastogenesis

“…About 60% of the intact bLF enters the small intestine after oral ingestion. 19 Therefore, we decided to use L-bLF to protect bLF from enzymatic digestion in the stomach. Recently, liposomalization of bLF was shown to improve resistance of bLF to gastric digestion, suggesting that oral administration of L-bLF could be a novel active constituent useful for preventive and therapeutic treatment of inflammatory diseases.…”

“…However, bLF is digested by the gastric juice and thus only 60% of the intact bLF enters the small intestine during oral administration. 19 Thus, specific enteric coating or specific delivery systems for bLF are needed for its effective oral administration. Liposomes prepared from naturally occurring biodegradable and nontoxic lipids have been proposed as efficient carriers for local delivery of therapeutic agents.…”

Bone Regeneration Is Promoted by Orally Administered Bovine Lactoferrin in a Rabbit Tibial Distraction Osteogenesis Model

“…Based on the results of a previous study [32], bovine lactoferrin is easily degraded to digestive enzymes such as pepsin or trypsin, and only 60% of the intact lactoferrin enters the intestine after oral ingestion in human beings. In our study, the degradation and the absorption ratios of bovine lactoferrin that were applied via oral administration in rabbits were not examined.…”