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通过调节交联剂与β-环糊精的摩尔比来提高姜黄素的载药量、释放度、溶解度和降低毒性。

Improved curcumin loading, release, solubility and toxicity by tuning the molar ratio of cross-linker to β-cyclodextrin.

机构信息

Department of Chemistry, Faculty of Science, University of Zanjan, Zanjan, Iran; Department of Pharmaceutical Biomaterials and Medical Biomaterials Research Center (MBRC), Faculty of Pharmacy, Tehran Univercity of Medical Sciences, Tehran, Iran.

Department of Medical Physics, School of Medicine, Tabriz University of Medical Science, Tabriz, Iran.

出版信息

Carbohydr Polym. 2019 Jun 1;213:70-78. doi: 10.1016/j.carbpol.2019.02.075. Epub 2019 Feb 22.


DOI:10.1016/j.carbpol.2019.02.075
PMID:30879691
Abstract

A novel β-cyclodextrin-based nanosponge (CDNS) was proposed as curcumin (CUR) delivery system improving pharmacokinetics and anticancer activity of CUR. The effect of molar ratio of Epiclon (EPI) as cross-linker and β-cyclodextrin (βCD) on the porosity, surface area, swelling ratio, CUR solubility and loading capacity, rate of drug release and selective toxicity of the CDNSs was fully investigated. The high degree of cross-linking led to the formation of mesoporous CDNS having high specific surface area and high loading capacity. All CUR-free CDNSs showed no toxicity against MCF 10A and 4T1 cells as normal and cancerous cells, respectively. While CDNSs-CUR exhibited selective toxicity against cancerous cells. In sum, high CUR aqueous solubility, significant loading and controllable release of the CUR, outstanding and selective toxicity against cancerous cells make CDNS8-CUR (EPI/βCD = 8) as promising candidate for further study in the cancer therapy.

摘要

一种新型的基于β-环糊精的纳米海绵(CDNS)被提出作为姜黄素(CUR)的递送系统,以提高 CUR 的药代动力学和抗癌活性。研究了交联剂 Epiclon(EPI)与β-环糊精(βCD)的摩尔比对纳米海绵的孔隙率、比表面积、溶胀比、CUR 溶解度和载药量、药物释放速率和选择性毒性的影响。高交联度导致形成具有高比表面积和高载药量的中孔 CDNS。所有不含 CUR 的 CDNS 对 MCF 10A 和 4T1 细胞(分别为正常细胞和癌细胞)均无毒性。而 CDNSs-CUR 对癌细胞表现出选择性毒性。总之,高 CUR 水溶解度、CUR 的显著载药量和可控释放、对癌细胞的优异和选择性毒性使 CDNS8-CUR(EPI/βCD=8)成为癌症治疗中进一步研究的有前途的候选药物。

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