Leonardi Dario, Lamas Maria C, Olivieri Alejandro C
IQUIR, CONICET, Faculty of Biochemical and Pharmaceutical Sciences, National University of Rosario, Suipacha 531, S2002LRK Rosario, Argentina.
J Pharm Biomed Anal. 2008 Nov 4;48(3):802-7. doi: 10.1016/j.jpba.2008.08.006. Epub 2008 Aug 15.
The loading of albendazole into biodegradable polymeric microparticles provides an attractive alternative to improve the drug dissolution rate. Experimental design and optimization techniques were implemented for the development of albendazole-chitosan microparticles using the ionic interaction method. The effect of seven different factors (chitosan concentration, pH of chitosan solution, stirring rate, stirring time, temperature, ionic agent and pH of ionic solutions) were studied on six responses: the yield, pH, morphology, size, dissolution rate and encapsulation efficiency of the microparticles. During the screening phase, the factors were evaluated at three levels each, in order to identify those which exert a significant effect. Multiple response simultaneous optimization by using the desirability function was then used to find experimental conditions where the system shows the most adequate results. The optimal conditions were found to be: NaOH as ionic agent at a pH value of 13.0, chitosan concentration, 0.50% (w/v) at a pH value of 1.0 and stirring rate, 1,000 rpm.
将阿苯达唑载入可生物降解的聚合物微粒中为提高药物溶解速率提供了一种有吸引力的替代方法。采用离子相互作用法,运用实验设计和优化技术来制备阿苯达唑-壳聚糖微粒。研究了七个不同因素(壳聚糖浓度、壳聚糖溶液的pH值、搅拌速率、搅拌时间、温度、离子剂和离子溶液的pH值)对微粒的六个响应指标的影响,这六个响应指标分别是:产率、pH值、形态、粒径、溶解速率和包封率。在筛选阶段,每个因素在三个水平上进行评估,以确定那些具有显著影响的因素。然后使用合意函数进行多响应同时优化,以找到系统显示出最理想结果的实验条件。发现最佳条件为:以氢氧化钠作为离子剂,pH值为13.0;壳聚糖浓度为0.50%(w/v),pH值为1.0;搅拌速率为1000转/分钟。