Modeling a system of phosphated cross-linked high amylose for controlled drug release. Part 2: physical parameters, cross-linking degrees and drug delivery relationships.
High amylose cross-linked to different degrees with sodium trimetaphosphate by varying base strength (2% or 4%) and contact time (0.5-4h) was evaluated as non-compacted systems for sodium diclophenac controlled release. The physical properties and the performance of these products for sodium diclophenac controlled release from non-compacted systems were related to the structures generated at each cross-linking degree. For samples at 2% until 2h the swelling ability, G' and eta* values increased with the cross-linking degree, because the longer polymer chains became progressively more entangled and linked. This increases water uptake and holding, favoring the swelling and resulting in systems with higher viscosities. Additionally, the increase of cross-linking degree should contribute for a more elastic structure. The shorter chains with more inter-linkages formed at higher cross-linking degrees (2%4h and 4%) make water caption and holding difficult, decreasing the swelling, viscosity and elasticity. For 2% samples, the longer drug release time exhibited for 2%4h sample indicates that the increase of swelling and viscosity contribute for a more sustained drug release, but the mesh size of the polymeric network seems to be determinant for the attachment of drug molecules. For the 4% samples, smaller meshes size should determine less sustained release of drug.
Cury
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Graduate Program in Pharmaceutical Sciences and Department of Drugs and Pharmaceuticals, Faculty of Pharmaceutical Sciences, São Paulo State University, UNESP, Rod. Araraquara-Jaú, km 1, CEP14801-902, Araraquara, SP, Brazil.
Castro
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Klein
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Evangelista
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RC
D000688:Amylose / Q000737:chemistry*; D002627:Chemistry, Physical; D003432:Cross-Linking Reagents / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004008:Diclofenac / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D008956:Models, Chemical; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry*; D012212:Rheology; D012995:Solubility; D013329:Structure-Activity Relationship
D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011122:Polyphosphates; D004008:Diclofenac; D000688:Amylose; C009293:trimetaphosphoric acid