A Mixed Micellar Formulation Suitable for the Parenteral Administration of Taxol

作者: Hayat Alkan‐Onyuksel , Suganthi Ramakrishnan , Hee‐Byung Chai , John M. Pezzuto

DOI: 10.1023/A:1018943021705

关键词: ChemistryDosage formChromatographyDilutionPhospholipidAqueous solutionLiposomeSolubilityDrug carrierMicelle

摘要: Taxol is a promising antitumor agent with poor water solubility. Intravenous administration of current taxol formulation in non-aqueous vehicle containing Cremophor EL may cause allergic reactions and precipitation upon aqueous dilution. In this study novel approach to formulate medium for i.v. delivery described. The drug solubilized bile salt (BS)/phospholipid (PC) mixed micelles. solubilization potential the micelles increased as total lipid concentration molar ratio PC/BS increased. Precipitation dilution was avoided by spontaneous formation drug-loaded liposomes from can be stored freeze-dried form achieve optimum stability, prepared simple just before administration. As judged panel cultured cell lines, cytotoxic activity retained when formulated mixed-micellar solution. Further, same potential, appeared less toxic than standard nonaqueous EL.

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