Sugar-branched-cyclodextrins as injectable drug carriers in mice.

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  • Additional Information
    • Source:
      Publisher: Informa Healthcare Country of Publication: England NLM ID: 7802620 Publication Model: Print Cited Medium: Print ISSN: 0363-9045 (Print) Linking ISSN: 03639045 NLM ISO Abbreviation: Drug Dev Ind Pharm Subsets: MEDLINE
    • Publication Information:
      Publication: London : Informa Healthcare
      Original Publication: New York, Dekker.
    • Subject Terms:
    • Abstract:
      The purpose of this study was to investigate stable complexation of drug in blood by sugar-branched-beta-cyclodextrins (beta-CDs) such as glucose (glu)- or galactose (gal)-branched-beta-CDs and the pharmacokinetic disposition of drug in sugar-branched-beta-CD complex. Complexation of steroidal drugs in sugar-branched-beta-CDs and their replacement by cholesterol were measured. The complexes of dexamethasone/glucosyl-beta-CDs (dexamethasone/glu-beta-CD or dexamethasone/glu-glu-beta-CD) were not replaced by cholesterol, which is a representative endogenous compound, whereas the complex of dexamethasone/beta-CD was replaced by cholesterol. The same results were obtained in steroidal drugs such as hydrocortisone, triamcinolone, and prednisolone. Thus, the use of glu-beta-CD and glu-glu-beta-CD permitted the stable complexation of the drug in water. Stability constants of dexamethasone/glu-glu-beta-CD and dexamethasone/gal-glu-beta-CD complexes are the same, which means that the sugar moiety of the side chain in beta-CD has little effect on stability constants. After the dexamethasone/gal-glu-beta-CD complex or the dexamethasone/glu-glu-beta-CD complex (dexamethasone: 1 mg/body) was administered intravenously to mice, dexamethasone concentrations in liver tissue and blood were measured. The dexamethasone/gal-glu-beta-CD complex (66.1 +/- 1.7 micrograms as dexamethasone/gram of liver tissue) was distributed to liver tissue significantly more than the dexamethasone/glu-glu-beta-CD (beta-CD) complex (59.9 +/- 1.0 micrograms as dexamethasone/gram of liver) at 30 min after administration (p < .05). Sugar-branched-beta-CD gave a water-soluble and stable complex for dexamethasone and changed the disposition of dexamethasone. Sugar-branched-beta-CDs are potentially excellent carriers for a steroidal injectable formulation.
    • Accession Number:
      0 (Carbohydrates)
      0 (Cyclodextrins)
      0 (Drug Carriers)
      0 (Steroids)
      7S5I7G3JQL (Dexamethasone)
      97C5T2UQ7J (Cholesterol)
    • Publication Date:
      Date Created: 19991222 Date Completed: 20000111 Latest Revision: 20190921
    • Publication Date:
      20240104
    • Accession Number:
      10.1081/ddc-100102286
    • Accession Number:
      10596356