Double-layered microparticles with enzyme-triggered release for the targeted delivery of water-soluble bioactive compounds to small intestine.
Double-layered microparticles for enzyme-triggered release in the gastrointestinal tract were prepared by spray-chilling a water/oil/water emulsion, which could be a promising candidate for the targeted delivery of water-soluble bioactive compounds. Based on response surface methodology, the optimum conditions for 2nd emulsifier content, concentration ratio of the single emulsion to the coating material, and dispersion fluid temperature were 201.5μmol, 0.30, and 10.1°C, respectively. Morphological characterisation using an FE-SEM indicated that double-layered microparticles with diameters of 7-10μm were spherical and possessed scores of inner droplets. Release profiles generated using in vitro digestion models revealed that the core of double-layered microparticles was gradually released by enzymatic degradation when exposed to the simulated intestinal environment. The accumulative release reached 59.8±0.2% within a residence time of 3h, whereas they were resistant to gastric release-stimuli, such as extremely low pH and pepsin (below 2.4±0.6%).
Department of Agricultural Biotechnology, Seoul National University, Seoul 151-921, Republic of Korea.
Kyung Min
KM
Park
R&D Center, Daesang Corporation, Gyeonggi-Do 467-813, Republic of Korea.
Ho
H
Sung
Department of Food Science and Technology, Department of Interdisciplinary Bio IT Materials, Seoul National University of Science and Technology, Seoul 139-743, Republic of Korea.
Seung Jun
SJ
Choi
Department of Agricultural Biotechnology, Seoul National University, Seoul 151-921, Republic of Korea; Center for Food and Bioconvergence, Research Institute for Agriculture and Life Sciences, Seoul National University, Seoul 151-742, Republic of Korea.
Young Jin
YJ
Choi
Department of Agricultural Biotechnology, Seoul National University, Seoul 151-921, Republic of Korea; Center for Food and Bioconvergence, Research Institute for Agriculture and Life Sciences, Seoul National University, Seoul 151-742, Republic of Korea. Electronic address: pschnag@snu.ac.kr.
Pahn-Shick
PS
Chang
D055252:Cell-Derived Microparticles; D045703:Emulsifying Agents / Q000737:chemistry*; D066298:In Vitro Techniques; D007421:Intestine, Small
D045703:Emulsifying Agents
Double-layered microparticle; Enzyme-triggered release; In vitro digestion model; Response surface methodology; Targeted delivery