CONTEXT Sesamol, a potential antioxidant with marked anticancer potential suffers from issues of extensive tissue distribution and local gastric irritation on oral administration. OBJECTIVE To develop multiunit gastro-retentive floating beads (S-FBs) for localised and prolonged release of sesamol to treat gastric cancers. MATERIALS AND METHODS S-FBs prepared using calcium carbonate, sodium alginate and hydroxypropylmethyl cellulose (HPMC) in different proportions, were characterised and evaluated in vivo in N-methyl-N-nitro-N-nitroguanidine-induced gastric cancer in rats. Single oral dose plasma pharmacokinetic study was also performed for free sesamol and S-FBs. RESULTS AND DISCUSSION Restraining sesamol in floating beads, significantly lowered the release (diffusion controlled) rate, increased t50% (31 times) and reduced its in vivo clearance (>1.5 times). Preclinical evaluation showed S-FBs (10 mg/kg) to be significantly better than free sesamol and better/equivalent to methotrexate (2 mg/kg). CONCLUSION Most of the natural phytochemical or antioxidants show pretreatment effectiveness. We, however, developed and established S-FBs for sustained curative effect.

中文翻译：

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载有芝麻酚的浮珠在胃癌中的作用：药代动力学和生化证据。

语境Sesamol是一种具有显着抗癌潜力的潜在抗氧化剂，在口服时会遭受广泛的组织分布和局部胃刺激的问题。目的开发多单位胃滞留性漂浮珠（S-FBs），用于局部和长期释放芝麻酚，以治疗胃癌。材料与方法使用碳酸钙，藻酸钠和羟丙基甲基纤维素（HPMC）以不同比例制备的S-FBs，在体内由N-甲基-N-硝基-N-硝基胍诱导的大鼠胃癌中进行了表征和评估。还对游离的芝麻酚和S-FBs进行了单次口服剂量的血浆药代动力学研究。结果与讨论抑制芝麻酚悬浮在浮珠中，可显着降低释放（扩散控制）速率，增加t50％（31倍）并降低其体内清除率（> 1.5倍）。临床前评估表明，S-FBs（10 mg / kg）显着优于游离芝麻酚，并且与甲氨蝶呤（2 mg / kg）更好/相当。结论多数天然植物化学物质或抗氧化剂具有预处理效果。但是，我们开发并建立了S-FB以获得持续的疗效。