title: Development and evaluation of alginate-chitosan gastric floating beads loading with oxymatrine solid dispersion.
abstract: Oxymatrine (OM) can be metabolized to matrine in gastrointestinal ileocecal valve after oral administration, which affects pharmacological activity and reduce bioavailability of OM. A type of multiple-unit alginate-chitosan (Alg-Cs) floating beads was prepared by the ionotropic gelation method for gastroretention delivery of OM. A solid dispersion technique was applied and incorporated into beads to enhance the OM encapsulation efficiency (EE) and sustain the drug release. The surface morphology and internal hollow structure of beads were evaluated using optical microscopy and scanning electron microscopy (SEM). The developed Alg-Cs beads were spherical in shape with hollow internal structure and had particle size of 3.49 ± 0.09 mm and 1.33 ± 0.09 mm for wet and dried beads. Over 84% of the optimized OM solid dispersion-loaded Alg-Cs beads were able to continuously float over the simulated gastric fluid for 12 h in vitro. The OM solid dispersion-loaded Alg-Cs beads showed drug EE of 67.07%, which was much higher than that of beads loading with pure OM. Compared with the immediate release of OM capsules and pure OM-loaded beads, the release of OM from solid dispersion-loaded Alg-Cs beads was in a sustained-release manner for 12 h. Prolonged gastric retention time of over 8.5 h was achieved for OM solid dispersion-loaded Alg-Cs floating beads in healthy rabbit in in vivo floating ability evaluated by X-ray imaging. The developed Alg-Cs beads loading with OM solid dispersion displayed excellent performance features characterized by excellent gastric floating ability, high drug EE and sustained-release pattern. The study illustrated the potential use of Alg-Cs floating beads combined with the solid dispersion technique for prolonging gastric retention and sustaining release of OM, which could provide a promising drug delivery system for gastric-specific delivery of OM for bioavailability enhancement.
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Ningxia Medical University , Yinchuan , People's Republic of China .|b Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University , Yinchuan , People's Republic of China , and.
authors.forename: Yanhua
authors.initials: Y
authors.lastname: Liu
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Ningxia Medical University , Yinchuan , People's Republic of China .
authors.forename: Lihong
authors.initials: L
authors.lastname: Chen
authors.affiliation: c The Affiliated Tumor Hospital of General Hospital of Ningxia Medical University , Yinchuan , People's Republic of China.
authors.forename: Chengming
authors.initials: C
authors.lastname: Zhou
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Ningxia Medical University , Yinchuan , People's Republic of China .|b Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University , Yinchuan , People's Republic of China , and.
authors.forename: Jianhong
authors.initials: J
authors.lastname: Yang
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Ningxia Medical University , Yinchuan , People's Republic of China .|b Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University , Yinchuan , People's Republic of China , and.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Hou
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Ningxia Medical University , Yinchuan , People's Republic of China .|b Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University , Yinchuan , People's Republic of China , and.
authors.forename: Wenping
authors.initials: W
authors.lastname: Wang
mesh_terms: D000464:Alginates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D000470:Alkaloids / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D000818:Animals; D048271:Chitosan / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems / Q000379:methods; D004353:Drug Evaluation, Preclinical; D005753:Gastric Mucosa / Q000378:metabolism*; D020723:Glucuronic Acid / Q000138:chemical synthesis / Q000493:pharmacokinetics; D006603:Hexuronic Acids / Q000138:chemical synthesis / Q000493:pharmacokinetics; D011807:Quinolizines / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011817:Rabbits; D011859:Radiography; D013270:Stomach / Q000000981:diagnostic imaging / Q000187:drug effects; D000093842:Matrines
chemical_list: D000464:Alginates; D000470:Alkaloids; D048271:Chitosan; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D011807:Quinolizines; C037573:oxymatrine; D000093842:Matrines
keywords: Alg-Cs gastric floating beads; OM; prolong gastric retention; solid dispersions; sustain drug release