针对口服给药体系如何保护药物分子免受人体内环境影响这一挑战, 采用乳化凝胶法设计合成了一种pH值敏感性的海藻酸钠(SA)-蒙脱石(MMT)复合微球MMT/SA, 用以负载抗癌药物盐酸阿霉素(DOX), 在保护药物分子的同时克服了胃肠道的生物化学屏障。探索了MMT处理工艺和合成配比的不同对微球形貌的影响, 最终控制微球尺寸在20 μm以内, 且分布均一。复合载药微球DOX/MMT/SA的载药率为14.7%, 在模拟人工胃液和人工肠液环境中表现出不同的药物缓释效果, 在模拟人工肠液中的累计释放率(31.7%)明显高于在人工胃液中的释放率(15.8%), 且对人结肠癌细胞有明显的杀伤效果。

Aiming at the challenge of how oral drug delivery systems protect drug molecules from environmental influences in human body, a pH value-sensitive sodium alginate-montmorillonite composite microsphere (MMT/SA) was synthesized by an emulsification gel method, which was used to load anticancer drug doxorubicin hydrochloride (DOX), and overcome the biochemical barrier of gastrointestinal tract while protecting drug molecules. The effect of raw material (MMT pretreatment and content) on the morphology of microspheres was investigated, and the size of microspheres with a uniform distribution was controlled to be 20 μm. The drug loading rate of DOX/MMT/SA is 14.7%, indicating different drug release effects in simulated gastric juice and artificial intestinal juice. The cumulative release rate of DOX/MMT/SA in simulated gastric juice (i.e., 31.7%) is greater than that in artificial gastric juice (i.e., 15.8%), and it has a killing effect on the cancer cells.