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将PEG2000进行活化后用来修饰透明质酸,得到PEG-HA,与美法仑键合得到前药PEG-HA-MEL。采用单因素实验考察相关因素对产率的影响,主要包括投料比、时间、催化剂和pH等,最终得到了各步骤的最优反应条件。用红外光谱、动态光散射和透射电镜对合成产物进行表征。结果表明:最优条件下,PEG活化的产率达到86.8%;PGE活性酯的产率达到84.2%;PEG-HA的产率为78.8%;PEG-HA-MEL的产率最高为62.3%。PEG-HA-MEL能在水溶液中形成胶束且其粒径在分布在120nm左右。
PEG2000 was used to modify hyaluronic acid to get PEG-HA, which was bonded with melphalan to obtain prodrug PEG-HA-MEL. The single factor experiment was used to investigate the influence of the relevant factors on the yield, including the feed ratio, time, catalyst and pH, finally obtained the optimal reaction conditions of each step. The synthesized products were characterized by FTIR, dynamic light scattering and transmission electron microscopy. The results showed that under the optimum conditions, the yield of PEG activation reached 86.8%, the yield of PGE active ester reached 84.2%, the yield of PEG-HA was 78.8%, and the yield of PEG-HA-MEL was 62.3%. PEG-HA-MEL can form micelles in aqueous solution with particle size distribution around 120nm.