Abstract
Lactoferrin (LF) is known to show various useful biological features such as antimicrobial, antiviral, antitumor and anti-inflammatory effects. However, orally administered LF undergoes enzymatic degradation in the gastrointestinal tract, resulting in extensive decrease of such functions. The purpose of this study is to develop a useful oral delivery system of LF. Also, chitosan (Ch) was adopted as a carrier because it is yielded abundantly and a safe polymer. LF-loaded Ch microparticles were produced by the emulsification-evaporation technique using sorbitan sesquioleate (SO-15) and sorbitan trioleate (SO-30) as surfactants. The resultant LF-loaded Ch microparticles were evaluated from the viewpoints of particle size, shape, drug content and in vitro release in the gastric and intestinal pHs. The selected LF-loaded microparticles (MS4) were coated with an enteric coating polymer, Eudragit L100 (EL-100). The resultant microparticles (E/MS4) were protected from the deformation in the gastric pH, and exhibited fairly appropriate release profiles of LF. Thus, enteric-coated MS4 was suggested to be possibly useful as an orally-taken delivery system of LF.
Highlights
Lactoferrin (LF) was found as a multifunctional iron-binding glycoprotein, and is widely contained in milk, saliva, tears, various exocrine secretions and neutrophil granules [1,2]
Chitosan (Ch, MW 100,000 – 200,000, deacetylation degree = 80%) and liquid paraffin were purchased from Wako Pure Chemical Industries, Ltd. (Osaka, Japan)
LF-loaded Ch microparticles were prepared with different formulations
Summary
Lactoferrin (LF) was found as a multifunctional iron-binding glycoprotein, and is widely contained in milk, saliva, tears, various exocrine secretions and neutrophil granules [1,2]. It exhibits antimicrobial [3,4], antiviral [5], antitumor [6], anti-inflammatory [7] and immunomodulation [8] activities. It works against microbes and viruses by direct binding [9,10,11,12,13,14] and by interaction with host cells [15] or activation of immune systems [16,17]. LF is used as a supplement in various countries
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