Water soluble poly(ethylene glycol) prodrug of silybin: Design, synthesis, and characterization

Peng Zhang, Hai Ye, Tao Min, Can Zhang*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

Silybin, the main component of Silymarin, is an antihepatotoxic agent. But it presents numerous challenges associated with its poor aqueous solubility which has been realized as the major problem in its dosage form development and clinical application. The objective of our study was to solubilize silybin by designing and synthesizing its aqueous soluble prodrug using high aqueous soluble polymeric carrier-poly(ethylene glycol) (PEG). A novel soluble silybin prodrug was synthesized with a linear PEG and succinic ester linkage, and was xtensively characterized using proton NMR, FTIR, and TPF-MS. Furthermore, the prodrug was evaluated for its drug loading capability which was 6.65% and the solubility was 800 mg/mL. The results indicate significantly higher solubility of the prodrug in comparison with silybin.

Original languageEnglish (US)
Pages (from-to)3230-3235
Number of pages6
JournalJournal of Applied Polymer Science
Volume107
Issue number5
DOIs
StatePublished - Mar 5 2008
Externally publishedYes

Keywords

  • Conjugated polymers
  • Drug delivery systems
  • Hydrophilic polymers
  • Synthesis
  • Water-soluble polymers

ASJC Scopus subject areas

  • Chemistry(all)
  • Surfaces, Coatings and Films
  • Polymers and Plastics
  • Materials Chemistry

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