Overweight and obesity, which contribute to various chronic diseases, are increasingly common conditions around the world. For the purpose of weight loss in patients with overweight and obesity, we developed a series of β-cyclodextrin functionalized cationic branched polyethylenimine as oral pharmaceutical agents to inhibit digestion and absorption of dietary lipids in vivo. Tuning the structural configuration, molecular weight, and side-chain length of the cationic polymers provided the polymer with effective inhibition of lipid absorption. Importantly, the cationic polymer significantly increased fecal elimination of bile acids, triglycerides and cholesterol by 6.3-, 4.8- and 5.0-fold higher than those of the control with high fat diet, respectively. Moreover, the polymer could reduce the plasma lipids and liver lipid level in mice. The cationic polymer exhibited low cytotoxicity and did not cause observable histological changes for normal tissue. Therefore, the cationic polymer showed effective and safe characteristics as an oral pharmaceutical agent for inhibiting lipid absorption. This work offers a new promising venue to control weight for patients with overweight and obesity.

超重和肥胖是导致各种慢性疾病的原因，在世界范围内越来越普遍。为了减轻超重和肥胖症患者的体重，我们开发了一系列β-环糊精官能化的阳离子支链聚乙烯亚胺作为口服药物来抑制体内饮食脂质的消化和吸收。调节阳离子聚合物的结构构型，分子量和侧链长度可有效抑制脂质吸收。重要的是，阳离子聚合物的粪便清除胆汁酸，甘油三酸酯和胆固醇的能力分别比高脂饮食对照组高6.3、4.8和5.0倍。而且，该聚合物可以降低小鼠的血浆脂质和肝脂质水平。阳离子聚合物表现出低细胞毒性，并且不会引起正常组织的可观察到的组织学变化。因此，该阳离子聚合物作为抑制脂质吸收的口服药物显示出有效和安全的特性。这项工作为控制超重和肥胖患者的体重提供了一个新的有希望的场所。