Marchais H, Benali S, Irache J M, Tharasse-Bloch C, Lafont O, Orecchioni A M
Laboratoire de Pharmacochimie et Biopharmacie (EA DRED 1295), Université de Rouen, Saint Etienne du Rouvray, France.
Drug Dev Ind Pharm. 1998 Sep;24(9):883-8. doi: 10.3109/03639049809088536.
Several formulations of poly(epsilon-caprolactone) (PCL), poly(lactic acid) (PLA), and poly(lactic-co-glycolic acid) (PLGA) nanocapsules containing phenylbutazone were prepared according to the interfacial deposition technique. These formulations differed in the type of polymer used to form the shell of the nanocapsules. Analysis of particle size distribution and encapsulation efficiency of the nanocapsules revealed that the type and molecular weight of polyester used were the main factors influencing these properties. PLA had the highest encapsulation efficiency with the best reproducibility. From in vitro release studies, a small amount of drug release was observed at pH 7.4. However, in the gastric medium, an important burst effect occurred and was highest with the PLGAs and lowest with PCL, suggesting that drug release from these systems is affected by the type of polymer and the environmental conditions. The two formulations of phenylbutazone-loaded nanocapsules should be evaluated based on PCL and PLA in vivo in order to determine to what extent they are able to reduce the local side effects of this drug.
根据界面沉积技术制备了几种含有苯基布他松的聚（ε-己内酯）（PCL）、聚乳酸（PLA）和聚乳酸-乙醇酸共聚物（PLGA）纳米胶囊制剂。这些制剂在用于形成纳米胶囊外壳的聚合物类型上有所不同。对纳米胶囊的粒径分布和包封率分析表明，所用聚酯的类型和分子量是影响这些性质的主要因素。PLA具有最高的包封率和最佳的重现性。体外释放研究表明，在pH 7.4时观察到少量药物释放。然而，在胃介质中，出现了重要的突释效应，PLGA的突释效应最高，PCL的突释效应最低，这表明这些系统中的药物释放受聚合物类型和环境条件的影响。应在体内对两种载苯基布他松纳米胶囊制剂进行基于PCL和PLA的评估，以确定它们能够在多大程度上降低该药物的局部副作用。
