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.
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Zhang et al. (2007) studied this question.
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