In order to achieve the delivery and controlled release of lactoferrin (LF), a biologically multifunctional protein, chitosan microparticles loaded with LF were prepared. Several types of chitosan microparticles containing LF were prepared by the w/o emulsification-solvent evaporation method, and the particle characteristics and release properties in JP 2nd fluid, pH 6.8, were examined. All kinds of microparticles were obtained at a yield of more than 75% (w/w). LF-loaded microparticles prepared by nonsonication and nonaddition of sulfate, named Ch-LF(N), showed high drug content, small particle size and spherical particle shape. Also, for release properties, Ch-LF(N) exhibited gradual drug release over 7 hr with less remaining in the microparticles. Considering the mucoadhesive properties of chitosan microparticles, Ch-LF(N) are suggested to be useful for gradual supply to topical diseased sites or for effective delivery to intestinal areas with abundant LF receptors.