Improved solubility and stability of rifampicin as an inclusion complex of acyclic cucurbit[n]uril

被引：9
作者：
Liu, Hui [1 ]
He, Zu-Zheng [1 ]
Yu, Lei [2 ]
Ma, Jun [3 ]
Jin, Xue-Pin [2 ]
机构：
[1] Wuhan Inst Technol, Sch Chem Engn & Pharm, Key Lab Green Chem Proc, Minist Educ, 693 Xiongchu Ave, Wuhan 430073, Peoples R China
[2] Wuhan Vocat Coll Software & Engn, Wuhan Drug Solubilizat & Delivery Technol Res Ctr, 117 Guanggu Blvd, Wuhan 430205, Peoples R China
[3] Wuhan Jinyintan Hosp, Dept Clin Lab, 1 Yintan Ave, Wuhan 430023, Peoples R China
来源：
JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY | 2021年 / 101卷 / 1-2期
基金：
中国国家自然科学基金;
关键词：
Tuberculosis; Rifampicin; Cucurbit[n]uril; Inclusion complex; Solubilization; CYCLODEXTRIN COMPLEXES; MOLECULAR CONTAINER; BETA-CYCLODEXTRIN; FORMULATION;
D O I：
10.1007/s10847-021-01093-3
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The poor solubility and low stability of rifampicin limited its therapeutic efficacy. One of the common strategies is to form an inclusion complex to address the problems. In this study, acyclic cucurbit[n]uril was used for encapsulation of rifampicin to form an inclusion complex. The inclusion complex was prepared by the kneading method and characterized by DSC, SEM, FT-IR, NMR, PXRD, and UV-Vis spectroscopy. The results confirmed the formation of 1:1 inclusion complex. The drug content was calculated to be 27.35 +/- 0.54%. The aqueous solubility of rifampicin was increased 20-fold by complexation with acyclic cucurbit[n]uril. Moreover, the thermo-stability and photo-stability of free rifampicin and inclusion complex were investigated by HPLC. Rifampicin was stabilized by encapsulating the piperazine ring in the cavity of acyclic cucurbit[n]uril. In addition, the MIC of free RIF and RIF.ACB were determined by using in vitro experiments. It was found that rifampicin complexed by acyclic cucurbit[n] uril exhibited similar antibacterial activities against strain H37Rv to rifampicin alone. [GRAPHICS] .
引用
收藏
页码：111 / 120
页数：10
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