title: Development of (-)-epigallocatechin-3-gallate (EGCG)-loaded enteric microparticles with intestinal mucoadhesive property.
abstract: The main purpose of the present investigation was to develop a novel enteric mucoadhesive formulation of (-)-epigallocatechin-3-gallate (EGCG), a green tea catechin, with the aim of avoiding its severe degradation in the gastrointestinal tract and therefore improving pharmacological effects. The EGCG-loaded microspheres (EGCG/MS), containing Eudragit(®) S100, were prepared with an emulsion solvent diffusion method in aqueous PVA solution. The EGCG/MS with a diameter of 16 μm exhibited pH-dependent controlled release of EGCG with limited initial burst release, and the Eudragit(®) S100-based MS also had moderate bioadhesive property in isolated small intestine of rats. There appeared to be marked degradation of EGCG in acidic solution (pH 1.2) and neutral buffer (pH 6.8) containing intestinal microsomal fraction, although significant improvement in chemical and metabolic stability of EGCG was observed in the EGCG/MS, possibly due to the controlled release and/or bioadhesion. From these findings, newly prepared EGCG/MS might be of clinical importance in both stabilizing and delivering EGCG for treatment of intestinal diseases.
authors.affiliation: Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. onoue@u-shizuoka-ken.ac.jp
authors.forename: Satomi
authors.initials: S
authors.lastname: Onoue
authors.forename: Masanori
authors.initials: M
authors.lastname: Ochi
authors.forename: Shizuo
authors.initials: S
authors.lastname: Yamada
mesh_terms: D000268:Adhesiveness; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry; D002392:Catechin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D004655:Emulsions; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000378:metabolism*; D008861:Microsomes / Q000378:metabolism; D008863:Microspheres; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D051381:Rats; D012997:Solvents / Q000737:chemistry
chemical_list: D000975:Antioxidants; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D011109:Polymethacrylic Acids; D012997:Solvents; C038300:methylmethacrylate-methacrylic acid copolymer; D002392:Catechin; D011142:Polyvinyl Alcohol; C045651:epigallocatechin gallate