A novel organic–inorganic microhybrids containing anticancer agent doxifluridine and layered double hydroxides: Structure and controlled release properties
A novel organic–inorganic microhybrids containing anticancer agent doxifluridine and layered double hydroxides: Structure and controlled release properties
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DOI：
10.1016/j.ces.2010.03.013
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发表时间：
2010-06
影响因子：
4.7
通讯作者：
De-Hai Pan;Hui Zhang;T. Zhang;X. Duan
中科院分区：
文献类型：
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作者：
De-Hai Pan;Hui Zhang;T. Zhang;X. Duan
对于完全受控的药物释放，重要的是要完全理解最终控制药物释放特性的层状双氢氧化物的微观结构和性质。本研究采用重构法制备了一系列新型的去氧氟尿苷插层镁铝水滑石（DFUR-LDH）微杂化材料。随着老化pH值从7.2增加到9.5，形成具有不同基底间距（d 003）的两个不同LDH相。d 0030. 82 nm的DFUR-LDHr 2. 0 p9.5具有不连续的板状形貌和多位点相互作用的层间排列，d 0031. 91 nm的DFUR-LDHr 1. 7 p7.2具有连续的蠕虫状形貌和可能的双层层间排列。体外释放实验表明，由于DFUR与LDH层间的相互作用较弱，前者的释药持续时间较长，初始释放速度略快。体外释药数据可用Bhaskar方程和Freundlich模型描述，表明DFUR-LDH微杂化材料的释药机制为颗粒扩散。此外，肠溶性聚合物修饰的DFUR-LDHr 1. 7 p7.2/L100微球在pH 1.2的盐酸溶液中释放不明显，但在pH 6.8和7.4的PBS中持续释放79%，表明微球在不同pH的介质中具有良好的控释性能，有望应用于肿瘤治疗的结肠靶向给药。
For fully controlled drug release, it is important to completely understand the microstructure and nature of the layered double hydroxide that ultimately control drug release properties. In this study, a series of novel doxifluridine intercalated Mg–Al-layered double hydroxide (DFUR–LDH) microhybrids were fabricated via the reconstruction method. With increasing aging pH values from 7.2 to 9.5, two different LDH phases with varied basal spacings (d003) are formed. The DFUR–LDHr1.7p7.2 with d0031.91nm presents continuous worm-like morphology and possible bilayer interlayer arrangement, while DFUR–LDHr2.0p9.5 with d0030.82nm possesses discontinuous plate-like morphology and multi-sites interacted interlayer arrangement. Consequently, the in vitro release shows that the former has much longer release duration and a little faster initial release due to the weaker interaction between DFUR and LDH layers than that of the latter. The in vitro release data can be well described by the Bhaskar equation and modified Freundlich model, revealing that the release mechanism of DFUR from DFUR–LDH microhybrids is heterogeneous particle diffusion. Furthermore, the enteric polymer modified DFUR–LDHr1.7p7.2/L100 microspheres present no obvious release in pH 1.2 HCl solution, but continuous release of 79% in pH 6.8 and 7.4 PBS, suggesting a readily controlled release behavior upon the varied medium pH and potential application in colon specific drug delivery in cancer therapy.