Czarnobaj K
Department of Physical Chemistry, The Medical University of Gdansk, Gdansk, Poland.
Drug Deliv. 2008 Nov;15(8):485-92. doi: 10.1080/10717540802321495.
The aim of the present study was to utilize the sol-gel method to synthesize different forms of xerogel matrices for drugs and to investigate how the synthesis conditions and solubility of drugs influence the change of the profile of drug release and the structure of the matrices. Silica xerogels doped with drugs were prepared by the sol-gel method from a hydrolyzed tetraethoxysilane (TEOS) solution containing two model compounds: diclofenac diethylamine, (DD)--a water-soluble drug or ibuprofen, (IB)--a water insoluble drug. Two procedures were used for the synthesis of sol-gel derived materials: one-step procedure (the sol-gel reaction was carried out under acidic or basic conditions) and the two-step procedure (first, hydrolysis of TEOS was carried out under acidic conditions, and then condensation of silanol groups was carried out under basic conditions) in order to obtain samples with altered microstructures. In vitro release studies of drugs revealed a similar release profile in two steps: an initial diffusion-controlled release followed by a slower release rate. In all the cases studied, the released amount of DD was higher and the released time was shorter compared with IB for the same type of matrices. The released amount of drugs from two-step prepared xerogels was always lower than that from one-step base-catalyzed xerogels. One-step acid-catalyzed xerogels proved unsuitable as the carriers for the examined drugs.
本研究的目的是利用溶胶-凝胶法合成不同形式的用于药物的干凝胶基质,并研究药物的合成条件和溶解度如何影响药物释放曲线的变化以及基质的结构。通过溶胶-凝胶法,由含有两种模型化合物的水解四乙氧基硅烷(TEOS)溶液制备掺杂药物的二氧化硅干凝胶:双氯芬酸二乙胺(DD)——一种水溶性药物,或布洛芬(IB)——一种水不溶性药物。采用两种方法合成溶胶-凝胶衍生材料:一步法(溶胶-凝胶反应在酸性或碱性条件下进行)和两步法(首先,TEOS在酸性条件下水解,然后硅醇基团在碱性条件下缩合),以获得具有不同微观结构的样品。药物的体外释放研究显示出两步相似的释放曲线:初始扩散控制释放,随后释放速率较慢。在所有研究的案例中,对于相同类型的基质,DD的释放量更高,释放时间比IB更短。两步法制备的干凝胶中药物的释放量总是低于一步法碱催化干凝胶中的释放量。一步法酸催化干凝胶被证明不适用于作为所研究药物的载体。