Molecular and Genetic Medicine

Formulation Study of Chitosan Microparticles Loaded with Lactoferrin

Abstract

Hiraku Onishi, Yoshiharu Machida, Ryuya Yoshida and Ken-ichi Watanabe

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.