title: Development of pH-sensitive pectinate/alginate microspheres for colon drug delivery.
abstract: The purposes of this study were to develop and evaluate calcium pectinate/alginate microspheres (PAMs) and to exploit their pH-sensitive properties for colon-targeted delivery of encapsulated cisplatin. PAMs were prepared using an electrospraying method. The PAMs, as cores, were then coated with Eudragit S100 using a polyelectrolyte multilayer coating technique in aqueous solution. The morphology of the microspheres was observed under scanning electron microscopy. In vitro drug release studies were performed in simulated gastrointestinal fluid, and the results indicated that approximately 5 % of the cisplatin was released from the Eudragit S100-coated PAMs, and 51 % of the cisplatin was released from the uncoated PAMs at 1 h. The release of cisplatin from the Eudragit S100-coated PAMs was more sustained in simulated gastric fluid than in simulated intestinal fluid due to the increased solubility of the coating polymer in media with pH >7.0. Drug release from the Eudragit S100-coated PAMs was best described by the Higuchi's square root model. From these results, it was concluded that Eudragit S100-coated PAMs are a potential carrier for delivery of cisplatin to the colon.
authors.affiliation: Department of Life Sciences, National Taiwan Ocean University, Keelung, Taiwan, ROC. fyhsu5565@gmail.com
authors.forename: Fu-Yin
authors.initials: FY
authors.lastname: Hsu
authors.forename: Ding-Syuan
authors.initials: DS
authors.lastname: Yu
authors.forename: Chun-Chiang
authors.initials: CC
authors.lastname: Huang
mesh_terms: D000464:Alginates / Q000138:chemical synthesis / Q000737:chemistry*; D002945:Cisplatin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D020099:Coated Materials, Biocompatible / Q000138:chemical synthesis / Q000737:chemistry; D003106:Colon / Q000378:metabolism; D004337:Drug Carriers / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005079:Excipients / Q000032:analysis / Q000737:chemistry; D005766:Gastrointestinal Contents; D020723:Glucuronic Acid / Q000138:chemical synthesis / Q000737:chemistry; D006603:Hexuronic Acids / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008422:Materials Testing; D008863:Microspheres; D010316:Particle Size; D010368:Pectins / Q000138:chemical synthesis / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry; D012995:Solubility
chemical_list: D000464:Alginates; D020099:Coated Materials, Biocompatible; D004337:Drug Carriers; D005079:Excipients; D006603:Hexuronic Acids; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D010368:Pectins; D020723:Glucuronic Acid; D002945:Cisplatin