A novel depot preparation of desferrioxamine-B: development of formulation principles |
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Authors: | Lowther N Sparks K Nicklin J Jin Y |
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Affiliation: | Drug Preformulation and Delivery Department, Ciba Pharmaceuticals (now Novartis Horsham Research Center), West Sussex, England. nicholas.lowther@pharma.novartis.com |
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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, drug loading, and particle size distribution of the depot preparation are described, and the physiochemical stability of an identified pilot formulation is assessed. |
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