Carbohydrate-based micelle clusters which enhance hydrophobic drug bioavailability by up to 1 order of magnitude

Xioazhong Qu, Vitaliy V. Khutoryanskiy, Ailsa Stewart, Samina Rahman, Brigitte Papahadjopoulos-Sternberg, Christine Dufès, Dave McCarthy, Clive G. Wilson, Robert Lyons, Katharine C. Carter, Andreas Schätzlein, Ijeoma F. Uchegbu

Research output: Contribution to journalArticle

86 Citations (Scopus)

Abstract

Amphiphilic chitosan-based polymers (Mw < 20 kDa) self-assemble in aqueous media at low micromolar concentrations to give previously unknown micellar clusters of 100-300 nm in size. Micellar clusters comprise smaller 10-30 nm aggregates, and the nanopolarity/drug incorporation efficiency of their hydrophobic domains can be tailored by varying the degree of lipidic derivatization and molecular weight of the carbohydrate. The extent of drug incorporation by these novel micellar clusters is 1 order of magnitude higher than is seen with triblock copolymers, with molar polymer/drug ratios of 1:48 to 1:67. On intravenous injection, the pharmacodynamic activity of a carbohydrate propofol formulation is increased by 1 order of magnitude when compared to a commercial emulsion formulation, and on topical ocular application of a carbohydrate prednisolone formulation, initial drug aqueous humor levels are similar to those found with a 10-fold dose of prednisolone suspension.
Original languageEnglish
Pages (from-to)3452-3459
Number of pages7
JournalBiomacromolecules
Volume7
Issue number12
DOIs
Publication statusPublished - 2006

Keywords

  • oside polymer
  • bioavailability
  • corticosteroid
  • prednisolone
  • central nervous system
  • binding capacity
  • micellar solution
  • aqueous solution
  • propofol
  • amphiphilic polymer
  • hydrophobic group
  • chitosan derivatives
  • pharmacology

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  • Cite this

    Qu, X., Khutoryanskiy, V. V., Stewart, A., Rahman, S., Papahadjopoulos-Sternberg, B., Dufès, C., McCarthy, D., Wilson, C. G., Lyons, R., Carter, K. C., Schätzlein, A., & Uchegbu, I. F. (2006). Carbohydrate-based micelle clusters which enhance hydrophobic drug bioavailability by up to 1 order of magnitude. Biomacromolecules, 7(12), 3452-3459. https://doi.org/10.1021/bm0604000