1999
DOI: 10.1081/ddc-100102283
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A Novel Depot Preparation of Desferrioxamine-B: Development of Formulation Principles

Abstract: This report describes the feasibility of simple oil-based depot formulations of a novel n-decanesulfonate salt of the iron chelator desferrioxamine-B. After subcutaneous administration in rodents, desferrioxamine-B n-decanesulfonate depot induces both (a) prolonged release of drug and (b) an increase of at least threefold to fourfold in iron excretion efficiency compared with the parent compound Desferal (desferrioxamine-B mesylate). Optimization experiments probing vehicle composition, surfactant loading, dru… Show more

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Cited by 4 publications
(4 citation statements)
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“…The drug has been assembled in liposomes [109], red cell ghosts [110], or oil vehicle after modifying the molecule to n-decanesulfonate salt [111]. This latter compound reached phase II development in humans but failed to show adequate efficacy [Porter J 1998] 15 .…”
Section: Research Perspectivesmentioning
confidence: 99%
“…The drug has been assembled in liposomes [109], red cell ghosts [110], or oil vehicle after modifying the molecule to n-decanesulfonate salt [111]. This latter compound reached phase II development in humans but failed to show adequate efficacy [Porter J 1998] 15 .…”
Section: Research Perspectivesmentioning
confidence: 99%
“…Considering that this therapy requires a high compromise from the patients, two approaches are being explored: (i) new techniques of DFO administration, and, ii) orally active Fe chelators. DFO administration routes tested include: twice daily subcutaneous bolus injections [54], hydroxyethyl starch DFO [55] and DFO depot [56]. Even when, at least the twice daily subcutaneous bolus injection regimen has shown good results, finding of an orally active Fe chelator is the main objective in this field.…”
Section: Searching For a Better Chelating Agentmentioning
confidence: 99%
“…Also, improved bioavailability and/or stability of DFO as well as decreased toxicity are observed. Formulations of DFO with n-decanesulfonate or poly(fumaric anhydride-co-sebacic anhydride) produced particles with increased efficiency in chelation treatment by slowing down the release of DFO from the particles [380,381]. In addition, microencapsulated formulations of L1 with Eudragit RS, RL and L90, and cellulose acetate phthalate have been developed to further improve its bioavailability [382].…”
Section: Examination Of Modified Chelators Complexing To Ironmentioning
confidence: 99%