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口服姜黄素包封于含 Eudragit 的脂质体的抗疟活性。

Antimalarial Activity of Orally Administered Curcumin Incorporated in Eudragit-Containing Liposomes.

机构信息

Nanomalaria Group, Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute of Science and Technology, Baldiri Reixac 10-12, ES-08028 Barcelona, Spain.

Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-Universitat de Barcelona), Rosselló 149-153, ES-08036 Barcelona, Spain.

出版信息

Int J Mol Sci. 2018 May 4;19(5):1361. doi: 10.3390/ijms19051361.

Abstract

Curcumin is an antimalarial compound easy to obtain and inexpensive, having shown little toxicity across a diverse population. However, the clinical use of this interesting polyphenol has been hampered by its poor oral absorption, extremely low aqueous solubility and rapid metabolism. In this study, we have used the anionic copolymer Eudragit S100 to assemble liposomes incorporating curcumin and containing either hyaluronan (Eudragit-hyaluronan liposomes) or the water-soluble dextrin Nutriose FM06 (Eudragit-nutriosomes). Upon oral administration of the rehydrated freeze-dried nanosystems administered at 25/75 mg curcumin·kg·day, only Eudragit-nutriosomes improved the in vivo antimalarial activity of curcumin in a dose-dependent manner, by enhancing the survival of all -infected mice up to 11/11 days, as compared to 6/7 days upon administration of an equal dose of the free compound. On the other hand, animals treated with curcumin incorporated in Eudragit-hyaluronan liposomes did not live longer than the controls, a result consistent with the lower stability of this formulation after reconstitution. Polymer-lipid nanovesicles hold promise for their development into systems for the oral delivery of curcumin-based antimalarial therapies.

摘要

姜黄素是一种抗疟化合物,易于获得且价格低廉,在不同人群中表现出的毒性很小。然而,由于其口服吸收差、水溶解度极低和代谢迅速,这种有趣的多酚的临床应用受到了阻碍。在这项研究中,我们使用阴离子共聚物 Eudragit S100 来组装含有姜黄素的脂质体,并含有透明质酸(Eudragit-透明质酸脂质体)或水溶性糊精 Nutriose FM06(Eudragit-nutriosomes)。在用水重新水化冻干纳米系统后经口给药,以 25/75mg 姜黄素·kg·天给药时,只有 Eudragit-nutriosomes 以剂量依赖的方式改善了姜黄素的体内抗疟活性,使所有感染的小鼠的存活率提高到 11/11 天,而给予相同剂量游离化合物时的存活率为 6/7 天。另一方面,用 Eudragit-透明质酸脂质体包封的姜黄素治疗的动物的存活时间不比对照组长,这一结果与该制剂再形成后的稳定性较低相一致。聚合物-脂质纳米囊泡有望开发成基于姜黄素的抗疟治疗的口服给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3449/5983818/e4ed5fc0806e/ijms-19-01361-g001.jpg

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