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.
Keywords: Obesity; Oral administration; Polyethylenimine; Weight loss; β-Cyclodextrin.
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