Construction of a water-soluble and photostable rubropunctatin/β-cyclodextrin drug carrier. Issue 20 (11th April 2019)

• Record Type: Journal Article
• Authors: Ren, Zhenzhen; Xu, Yanan; Lu, Zhenxin; Wang, Zhenzhen; Chen, Chengqun; Guo, Yanghao; Shi, Xianai; Li, Feng; Yang, Jianmin; Zheng, Yunquan
• Is Part Of: RSC advances. Volume 9:Issue 20(2019)
• Page Start: 11396
• Page End: 11405
• Publication Date: 2019-04-11
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c9ra00379g
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : The purpose of the current study was to construct a β-cyclodextrin drug carrier for rubropunctatin to improve its water solubility and light stability for future cytotoxicity studies. Abstract : The purpose of the current study was to construct a β-cyclodextrin drug carrier for rubropunctatin to improve its water solubility and light stability for future cytotoxicity studies. The inclusion complexation behavior of rubropunctatin with β-cyclodextrin was investigated using FESEM, FT-IR and XRD. A molecular docking study was performed to elucidate the most probable inclusion structure. The inclusion complex could be completely dispersed in water and had a small size of 121.87 ± 2.13 nm ( n = 3), a good PDI (0.320 ± 0.017), and an acceptable potential value of −27.7 ± 0.32 mV ( n = 3). Furthermore, the stability of the rubropunctatin in water under light irradiation was found to be greatly enhanced after being encapsulated in cyclodextrin, and it exhibited a retention rate of over 70% vs. 10.17%. In addition, the cytotoxicity of the inclusion complex was evaluated by MTT assay and Annexin V-FITC/PI detection using cervical adenocarcinoma HeLa cells. The results showed that the inclusion complex had comparable toxicity compared to rubropunctatin solubilized with 0.4% DMSO. More importantly, the formation of the inclusion complex contributed greatly to the intensification of the bioavailability of rubropunctatin because the use of organic solvent was avoided.