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

✍ Scribed by Peng Zhang; Hai Ye; Tao Min; Can Zhang

• Publisher: John Wiley and Sons
• Year: 2007
• Tongue: English
• Weight: 172 KB
• Volume: 107
• Category: Article
• ISSN: 0021-8995
• DOI: 10.1002/app.27450

✦ Synopsis

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 extensively characterized using proton NMR, FTIR, and TOF‐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. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008