增强型介孔沸石斯普赛石中抗癌药物莱特罗唑的溶解性。
Enhanced dissolution of anticancer drug letrozole from mesoporous zeolite clinoptilolite.
发表日期:2023 Sep 01
作者:
Radovan Kukobat, Ranko Škrbić, Fernando Vallejos-Burgos, Elisa Mercadelli, Davide Gardini, Laura Silvestroni, Chiara Zanelli, Laura Esposito, Dragana Stević, Suzana Gotovac Atlagić, Darko Bodroža, Žarko Gagić, Saša Pilipović, Biljana Tubić, Nataša Bubić Pajić
来源:
CLINICAL PHARMACOLOGY & THERAPEUTICS
摘要:
高生物利用度的药物输送系统对直接吸附在多孔载体上的抗癌药物的高溶解是不可或缺的。我们报道了在表面活化后将抗癌药物雷洛唑(LTZ)直接吸附/装载到伊利石(CLI)沸石上。体外实验表明,LTZ从CLI沸石中的溶解度在23小时内达到95%,在酸性介质中溶解速度比纯LTZ分子的溶解速度更快。快速溶解是因为LTZ均匀暴露于CLI沸石的外表面,易于与溶剂接触溶解。另一方面,LTZ分子隐藏在体积相中,呈现缓慢的溶解速率。CLI / LTZ吸附能的小正值为0.06 eV,表明在水介质中释放过程是有利的。CLI / LTZ系统的主要优点是其快速发挥作用和高生物利用度。本研究展示了从CLI沸石中增强溶解性较差的LTZ的溶解的可能性,这对进一步发展药物输送系统具有潜在的前景。版权©2023 Elsevier公司。保留所有权利。
High dissolution of anticancer drugs directly adsorbed onto porous carriers is indispensable for the development of drug delivery systems with high bioavailability. We report direct adsorption/loading of the anticancer drug letrozole (LTZ) onto the clinoptilolite (CLI) zeolite after the surface activation.In vitroLTZ dissolution from the CLI zeolites reached 95 % after 23 h in an acidic medium, being faster than the dissolution of the pure LTZ molecules. Fast dissolution occurs due to uniform exposure of the LTZ onto the external surface of the CLI zeolites, being accessible to the solvent for dissolution. On the other hand, the LTZ molecules were hidden in the bulk phase, giving a slow dissolution rate. Small positive value of the CLI/LTZ adsorption energy of 0.06 eV suggests that the release process is favourable in aqueous media. The main merit of the CLI/LTZ system is its quick onset of action and high bioavailability. This work demonstrates a possibility of enhancement of the dissolution of poorly soluble LTZ from the CLI zeolite, being promising for the further development of drug delivery systems.Copyright © 2023 Elsevier Inc. All rights reserved.