负载于粘土纳米复合材料上的具有抗菌活性的香芹酚前药
Carvacrol Prodrugs with Antimicrobial Activity Loaded on Clay Nanocomposites.
作者信息
Eusepi Piera, Marinelli Lisa, García-Villén Fátima, Borrego-Sánchez Ana, Cacciatore Ivana, Di Stefano Antonio, Viseras Cesar
机构信息
Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, Chieti, 66100 Abruzzo, Italy.
Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, 18071 Granada, Spain.
出版信息
Materials (Basel). 2020 Apr 10;13(7):1793. doi: 10.3390/ma13071793.
BACKGROUND
Carvacrol, an essential oil with antimicrobial activity against a wide range of pathogens, and its water soluble carvacrol prodrugs (WSCP1-3) were intercalated into montmorillonite (VHS) interlayers to improve their stability in physiological media and promote their absorption in the intestine.
METHODS
Intercalation of prodrugs by cation exchange with montmorillonite interlayer counterions was verified by X-ray powder diffraction and confirmed by Fourier transform infrared spectroscopy and thermal analysis.
RESULTS
In vitro release studies demonstrated that montmorillonite successfully controlled the release of the adsorbed prodrugs and promoted their bioactivation only in the intestinal tract where carvacrol could develop its maximum antimicrobial activity. The amount of WSCP1, WSCP2, and WSCP3 released from VHS were 38%, 54%, and 45% at acid pH in 120 min, and 65%, 78%, and 44% at pH 6.8 in 240 min, respectively.
CONCLUSIONS
The resultant hybrids successfully controlled conversion of the prodrugs to carvacrol, avoiding premature degradation of the drug.
背景
香芹酚是一种对多种病原体具有抗菌活性的精油，其水溶性香芹酚前药（WSCP1 - 3）被插层到蒙脱石（VHS）的层间，以提高它们在生理介质中的稳定性并促进其在肠道中的吸收。
方法
通过与蒙脱石层间抗衡离子进行阳离子交换来插层前药，这通过X射线粉末衍射得到验证，并通过傅里叶变换红外光谱和热分析得到证实。
结果
体外释放研究表明，蒙脱石成功地控制了吸附前药的释放，并且仅在香芹酚能够发挥其最大抗菌活性的肠道中促进其生物活化。在120分钟内，VHS释放的WSCP1、WSCP2和WSCP3在酸性pH下分别为38%、54%和45%，在pH 6.8下240分钟内分别为65%、78%和44%。
结论
所得的杂化物成功地控制了前药向香芹酚的转化，避免了药物的过早降解。
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