title: Novel Pullulan-Eudragit® S100 blend microparticles for oral delivery of risedronate: formulation, in vitro evaluation and tableting of blend microparticles.
abstract: Polymer blends have been considered a promising strategy to tailor drug release. In order to achieve gastroresistance and controlled release, Pullulan, a polysaccharide, and Eudragit® S100, an enteric polymer were selected to prepare microparticles for oral delivery of risedronate, an antiresorptive drug associated with GI tract injuries. Blend microparticles were prepared by spray-drying technique at 3 Pullulan and Eudragit® S100 ratios (MP2:1, MP1:1 and MP1:2) and were characterized in terms of yield, particle size, encapsulation efficiency, morphology, moisture content, flowability and in vitro drug release profiles. Microparticles presented yields between 31 and 42%, encapsulation efficiencies close to 100%, moisture contents lower than 11%, particle size ranging from 2.9 to 4.8 μm and narrow distribution. In the gastric medium, MP1:2 showed the best gastroresistance profile. In the intestinal fluid, all samples were able to prolong drug release. MP1:2 was compressed into tablets with or without polyvinylpyrrolidone. Both tableted microparticles could be obtained with acceptable average weights, drug content close to 100%, sufficient hardness and low friability. In vitro studies showed that tablets maintained the gastroresistance observed for microparticles and were also able to prolong risedronate release. In conclusion, Pullulan/Eudragit® S100 microparticles are promising alternatives for the oral delivery of risedronate in the future.
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Aline
authors.initials: A
authors.lastname: de Arce Velasquez
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Luana Mota
authors.initials: LM
authors.lastname: Ferreira
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Mônica Fabiele Lorensi
authors.initials: MF
authors.lastname: Stangarlin
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Cristiane de Bona
authors.initials: Cde B
authors.lastname: da Silva
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Clarice Madalena Bueno
authors.initials: CM
authors.lastname: Rolim
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil. Electronic address: leticiacruz@smail.ufsm.br.
authors.forename: Letícia
authors.initials: L
authors.lastname: Cruz
mesh_terms: D000284:Administration, Oral; D002021:Buffers; D002626:Chemistry, Pharmaceutical; D012968:Etidronic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D005936:Glucans / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012212:Rheology; D000068296:Risedronic Acid; D012996:Solutions; D013607:Tablets
chemical_list: D002021:Buffers; D005936:Glucans; D011109:Polymethacrylic Acids; D012996:Solutions; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; C009109:pullulan; D000068296:Risedronic Acid; D012968:Etidronic Acid
keywords: Blending; Eudragit S100; Microparticles; Oral delivery; Pullulan; Risedronate