Study on synthesizing the complex of sorafenib with 2-hydroxypropyl-β-cyclodextrin to enhance the anticancer activity of the drug substance

被引:2
作者
Bui, Van Cuong [1 ]
Pham, Thi Lan [1 ,2 ]
Nguyen, Thi Lam [1 ,2 ]
Tran, Thi Kim Chinh [1 ,2 ]
Le, Thi My Hanh Le [1 ]
Vu, Xuan Minh [1 ]
Le-Deygen, Irina M. [3 ]
Nguyen, Chau Anh [1 ]
Mai, Thanh Tung [4 ]
Shuib, Raa Khimi [5 ]
机构
[1] Vietnam Acad Sci & Technol, Inst Trop Technol, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam
[2] Vietnam Acad Sci & Technol, Grad Univ Sci & Technol, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam
[3] Lomonosov Moscow State Univ, Dept Chem Enzymol, 1,11b Leninkie Gory, Moscow 119991, Russia
[4] Hanoi Univ Sci & Technol, 1 Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam
[5] Univ Sains Malaysia, Sch Mat & Mineral Resources Engn, USM Engn Campus, Nibong Tebal 14300, Pulau Pinang, Malaysia
关键词
Anti-cancer; cyclodextrin; drug carrier; inclusion complex; solubility; sorafenib;
D O I
10.1515/pac-2024-0024
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
This study aims to synthesize inclusion complex derived from sorafenib (Sor) and hydroxypropyl-beta-cyclodextrin (HP beta CD) (denoted as [Sor-HP beta CD]). The complex of Sor with HP beta CD has been synthesized in a mixed solvent of H2O-DMSO, with a DMSO volume fraction of 80 %. The results of FTIR, DSC, and UV-Vis analysis have demonstrated the success of complex formation: the intensity of some characteristic peaks for the Sor binding decreased after complex formation, indicating that a part of the guest molecule has entered the cavity of the HP beta CD molecule. This is further supported by the DSC analysis results, showing the transformation of the complex's crystalline form to an amorphous form. The phase solubility diagram study also indicates that the solubility of Sor significantly increases, approximately 7 times higher than pure Sor, after complex formation. The results of the cell growth inhibition activity test in a water environment show that the complex inhibits the growth of Hep-G2 cells with an IC50 value of 62.4 mu g/mL, while pure Sor does not exhibit activity as it is practically insoluble in water.
引用
收藏
页码:1101 / 1110
页数:10
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