当前位置: X-MOL 学术ChemMedChem › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Injectable Hydrogel of Vitamin B9 for the Controlled Release of Both Hydrophilic and Hydrophobic Anticancer Drugs
ChemMedChem ( IF 3.4 ) Pub Date : 2018-11-05 , DOI: 10.1002/cmdc.201800562
Aditi Panja 1 , Sujoy Das 1 , Atanu Chakraborty 2 , Priyadarshi Chakraborty 1 , Suman Pal 2 , Arun K. Nandi 1
Affiliation  

Folic acid (FA), vitamin B9, is a good receptor of drugs triggering cellular uptake via endocytosis. FA is sparingly soluble in water. Herein, a new approach for the formation of FA hydrogel by the hydrolysis of glucono‐δ‐lactone in PBS buffer under physiological conditions has been reported. The gel has a fibrillar network morphology attributable to intermolecular H‐bonding and π‐stacking interactions. The thixotropic property of the gel is used for the encapsulation of both hydrophilic [doxorubicin (DOX)] and hydrophobic [camptothecin (CPT)] drugs. The loading of DOX and CPT into the gel is attributed to the H‐bonding interaction between FA and drugs. The release of DOX is sustainable at pH 4 and 7, and the Peppas model indicates that at pH 7 the diffusion of the drug is Fickian but it is non‐Fickian at pH 4. The release of CPT is monitored by fluorescence spectroscopy, which also corroborates the combined release of both drugs. The metylthiazolyldiphenyltetrazolium bromide assay of FA hydrogel demonstrates nontoxic behavior and that the cytotoxicity of the DOX‐loaded FA hydrogel is higher than that of pure DOX, with a minimal effect on normal cells.

中文翻译:

注射用维生素B9的水凝胶可控释亲水性和疏水性抗癌药

叶酸(FA),维生素B 9,是通过内吞作用触发细胞摄取的药物的良好受体。FA微溶于水。在此,已经报道了在生理条件下通过PBS缓冲液中的葡糖酸-δ-内酯水解形成FA水凝胶的新方法。凝胶具有纤维状网络形态,这归因于分子间的H键和π堆积相互作用。凝胶的触变性用于亲水性[阿霉素(DOX)]和疏水性[喜树碱(CPT)]药物的封装。凝胶中DOX和CPT的负载归因于FA和药物之间的H键相互作用。DOX的释放在pH 4和7时是可持续的,Peppas模型表明,在pH 7时,药物的扩散是Fickian的,但在pH 4时是非Fickian的。CPT的释放通过荧光光谱法进行监测,这也证实了两种药物的联合释放。FA水凝胶的溴化甲基噻唑基二苯基四唑鎓测定显示出无毒行为,并且载有DOX的FA水凝胶的细胞毒性高于纯DOX,对正常细胞的影响最小。
更新日期:2018-11-05
down
wechat
bug