Arias José L, Linares-Molinero Fernando, Gallardo Visitación, Delgado Angel V
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Spain.
Eur J Pharm Sci. 2008 Mar 3;33(3):252-61. doi: 10.1016/j.ejps.2007.12.005. Epub 2007 Dec 23.
The aim of this study is to develop a detailed investigation of the capabilities of carbonyl iron/poly(butylcyanoacrylate) (core/shell) particles for the loading and release of 5-Fluorouracil and Ftorafur. The anionic polymerization procedure, used to obtain poly(alkylcyanoacrylate) nanoparticles for drug delivery, was followed in the synthesis of the composite particles, except that the polymerization medium was a carbonyl iron suspension. The influence of the two mechanisms of drug incorporation (entrapment in the polymeric network and surface adsorption) on the drug loading and release profiles were investigated by means of spectrophotometric and electrophoretic measurements. The optimum loading conditions were ascertained and used to perform drug release evaluations. Among the factors affecting drug loading, both pH and drug concentration were found to be the main determining ones. For both drugs, the release profile was found to be biphasic, since the drug adsorbed on the surface was released rather rapidly (close to 100% in 1h), whereas the drug incorporated in the polymer matrix required between 10 and 20h to be fully released. The kinetics of the drug release from the core/shell particles was mainly controlled by the pH of the release medium, the type of drug incorporation, and the amount of drug loaded.
本研究的目的是对羰基铁/聚(氰基丙烯酸丁酯)(核/壳)颗粒负载和释放5-氟尿嘧啶及替加氟的能力展开详细研究。用于制备药物递送用聚(烷基氰基丙烯酸酯)纳米颗粒的阴离子聚合程序,在复合颗粒的合成中也被采用,只是聚合介质为羰基铁悬浮液。通过分光光度法和电泳测量研究了两种药物掺入机制(包埋于聚合物网络和表面吸附)对药物负载和释放曲线的影响。确定了最佳负载条件并用于进行药物释放评估。在影响药物负载的因素中,pH值和药物浓度均被发现是主要的决定因素。对于两种药物,释放曲线均呈双相,因为吸附在表面的药物释放相当迅速(1小时内接近100%),而包埋在聚合物基质中的药物则需要10至20小时才能完全释放。核/壳颗粒药物释放的动力学主要受释放介质的pH值、药物掺入类型和药物负载量的控制。