Synthesis and Characterization for PEG-SuccinylAmino Acidyl-Pterostilbene Conjugates and in vitro Release of Peterogtilbene

By : Yue Zhang, Shuchun Zhao, Xianxian Shi, Aibing Chen, Hua Zhao, Hongxia Du

Page No: 393-405

Abstract
Pterostilbene, as attracting much attention for its diversified pharmacological activities including anti-inflammation and anti-oxidation, has great potential in the pharmaceutical application. In this study, PEG–conjugated pterostilbene was designed to improve the poor solubility and stability of pterostilbene aiming to achieve the controlled release. Twelve different types of amino acid and succinyl were used as the linking arm between PEG and pterostilbene in the prepared conjugates. The prepared PEG-amino acidyl-pterostilbene conjugates were characterized by 1 HNMR, IR and DSC. Solubility, free pterostilbene and loading capability of the prepared conjugates were determined by UV and HPLC method. In vitro release of the conjugates was also evaluated by using dialysis method. The results indicated that Twelve different types of PEG-amino acidyl-pterostilbene conjugates were successfully synthesized. Water solubility of the conjugates were all greater than 600 mg·mL-1. The prepared PEG conjugates showed good ability of controlled release. Of all the prepared conjugates, PEG[1]succinyl-lysine-pterostilbene showed the best performance in in vitro release with lipase and PEG-succinyl-lysine-pterostilbene showed the best performance in in vitro release without lipase. The highest accumulative release rate of PEG-succinyl-lysine-pterostilbene was of 47% with lipase while 40% of PEG-succinyl-methionine-pterostilbene without lipase at pH 7.4 buffer within 72 h.

Authors :
Yue Zhang, Shuchun Zhao, Xianxian Shi, Aibing Chen, Hua Zhao and Hongxia Du : School of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, China.