title: Preparation and characterisation of phenytoin-loaded alginate and alginate-chitosan microparticles.
abstract: We aimed to prepare and investigate microparticles with the varying contents of calcium gelling ion, loaded with phenytoin, a standard antiepileptic agent, in its acidic form. Two different methods of alginate-based microparticles preparation were used: with and without treatment with chitosan. Furthermore, two standard procedures, the one-stage and the two-stage, were applied. Microparticle size of 12 one-stage formulations ranged from 466 to 636 mum. Both types of formulations, chitosan-treated and nontreated, appeared to be highly loaded with the model drug (91-96%). The chitosan-coated alginate-based microparticles prepared by the one-stage procedure exhibited kinetics of phenytoin liberation comparable to a similar sustained release system that had been tested at pH 6.8, as published earlier. As the gel erosion of alginate-based microparticles should be potentiated by the higher pH (used in the present study at pH 7.4), the most favorable of 12 formulations, with the liberation half-time of about 2 hr, seemed to be eligible for further modifications. Counterintuitively, the applied two-stage procedure did not appear to beneficially affect the dissolution behavior of phenytoin when tested in two formulations, which makes further modifications necessary.
authors.affiliation: DCP Hemigal, Leskovac, Serbia.
authors.forename: Nebojsa D
authors.initials: ND
authors.lastname: Cekić
authors.forename: Snezana D
authors.initials: SD
authors.lastname: Savić
authors.forename: Jela
authors.initials: J
authors.lastname: Milić
authors.forename: Miroslav M
authors.initials: MM
authors.lastname: Savić
authors.forename: Zarko
authors.initials: Z
authors.lastname: Jović
authors.forename: Marija
authors.initials: M
authors.lastname: Malesević
mesh_terms: D000464:Alginates / Q000737:chemistry*; D000927:Anticonvulsants / Q000737:chemistry / Q000493:pharmacokinetics; D002122:Calcium Chloride / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D004339:Drug Compounding; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D008863:Microspheres; D010316:Particle Size; D010672:Phenytoin / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000464:Alginates; D000927:Anticonvulsants; D006603:Hexuronic Acids; D010672:Phenytoin; D020723:Glucuronic Acid; D048271:Chitosan; D002122:Calcium Chloride