i3S - Institute for Research and Innovation in Health/INEB -Institute of Biomedical Engineering (INEB), University of Porto, Portugal; ICBAS - Institute of Biomedical Sciences Abel Salazar, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal.
i3S - Institute for Research and Innovation in Health/INEB -Institute of Biomedical Engineering (INEB), University of Porto, Portugal.
Mater Sci Eng C Mater Biol Appl. 2020 Jul;112:110920. doi: 10.1016/j.msec.2020.110920. Epub 2020 Apr 3.
Chitosan was grafted with O-methyl-O'-succinylpolyethylene glycol and oleic acid after a two-step carbodiimide coupling. The structural and physicochemical characterization of the compounds confirmed the successful conjugation of the hydrophilic and hydrophobic moieties to the chitosan backbone. The amphiphilic chitosan derivative obtained allowed the formation of polymeric micelles with an average size of 140 nm, a polydispersity index <0.234, and a positive superficial charge. Camptothecin, used as a model hydrophobic drug, was successfully carried into the polymeric micelles with an encapsulation efficiency of 78%. The in vitro drug release was evaluated in simulated gastrointestinal fluids, exhibiting a low release of camptothecin in gastric media and a controlled release in intestinal fluids. Furthermore, it was demonstrated that chitosan micelles were able to stabilize camptothecin, protecting up to 75% of the drug from hydrolysis, preserving its active lactone form. This new chitosan amphiphilic system exhibits great potential to load hydrophobic drugs, acting as a promising delivery system.
壳聚糖经两步碳二亚胺偶联法接枝 O-甲基-O'-琥珀酰聚乙二醇和油酸。化合物的结构和物理化学特性证实了亲水性和疏水性部分成功连接到壳聚糖主链上。所得的两亲性壳聚糖衍生物可形成平均粒径为 140nm、多分散指数<0.234、表面带正电荷的聚合物胶束。喜树碱被用作模型疏水性药物，成功地被包封到聚合物胶束中，包封效率为 78%。在模拟胃肠道液中进行了体外药物释放评价，在胃介质中表现出喜树碱的低释放，而在肠液中则表现出控制释放。此外，还证明壳聚糖胶束能够稳定喜树碱，使高达 75%的药物免于水解，保持其活性内酯形式。这种新的壳聚糖两亲性系统具有负载疏水性药物的巨大潜力，可作为一种有前途的药物递送系统。
