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Stability of Bovine Lactoferrin in Luminal Extracts and Mucosal Homogenates from Rat Intestine: A Prelude to Oral Absorption
Author(s) -
Yao Xudong,
Bunt Craig,
Cornish Jillian,
Quek SiewYoung,
Wen Jingyuan
Publication year - 2014
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12360
Subject(s) - lactoferrin , ileum , proteolysis , trypsin , proteases , digestion (alchemy) , small intestine , biochemistry , biology , jejunum , duodenum , bioavailability , chemistry , enzyme , medicine , pharmacology , chromatography
Oral delivery is the most common method for bovine lactoferrin ( bL f) administration. However, the presence of proteolytic enzymes in the stomach and intestine limits the effective absorption of bL f within the gastrointestinal ( GI ) tract. To determine the extent of bL f proteolysis, several digestion models were developed using luminal extracts and mucosal homogenates isolated from four regions of rat intestine: duodenum, jejunum, ileum, and proximal colon. The kinetics of bL f degradation followed a pseudo‐first‐order rate, and almost complete hydrolysis of bL f was observed in the luminal extracts, indicating that bL f is more susceptive to luminal peptidases rather than mucosal enzymes. Moreover, a significant reduction in bL f proteolysis was observed in the presence of soybean trypsin inhibitor ( SBTI ), bestatin, and bacitracin, suggesting that there exist trypsin‐like and aminopeptidase‐like proteases, which play a key role in the degradation of bL f in the intestine. Lactoferrin was then encapsulated in several lipid‐based delivery systems including liposomes and solid lipid particles ( SLP s) with polymer modification, showing at least 50% of intact bL f remaining after 6 h of digestion compared with native bL f. These findings suggest that particle encapsulation may modulate protein digestion and possibly achieve sufficient oral bioavailability of bL f.