Gürkan H, Yalabik-Kaş H S, Sumnu M, Hincal A A
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Hacettepe, Ankara, Turkey.
J Microencapsul. 1987 Jan-Mar;4(1):39-46. doi: 10.3109/02652048709031582.
Targeting of drugs by microspheres, nanoparticles and liposomes is intended to increase the selective targeting to specific organs and to reduce their side effects. Streptomycin sulphate, a tuberculostatic antibiotic, is used as the active principle in this study. The aim is to accumulate the loaded microspheres in the lungs. The release of drugs associated with microsphere carriers has been found to be dependent on a number of factors. The aim of the investigation was to study the influence of the extent and nature of cross-linking, the type and the amount of the matrix material on the release characteristics of streptomycin sulphate microspheres. Human serum albumin and gelatin (Type B) were used as two different matrix materials. The crosslinking agents used were 2,3-butanedione and formaldehyde at different concentrations, and variable duration times. The in vitro release of streptomycin sulphate from microspheres is characteristically biphasic, with an initial fast release (the 'burst effect'), followed by a much slower release. Alteration in the characteristics of drug-loaded microspheres result in significant changes in the second (slow) phase of release. The release profiles of the different formulations has been studied and evaluated kinetically.
通过微球、纳米颗粒和脂质体实现药物靶向旨在增强对特定器官的选择性靶向并减少其副作用。硫酸链霉素是一种抑菌抗生素，在本研究中用作活性成分。目的是使负载的微球在肺部蓄积。已发现与微球载体相关的药物释放取决于多种因素。该研究的目的是研究交联程度和性质、基质材料的类型和用量对硫酸链霉素微球释放特性的影响。人血清白蛋白和明胶（B型）用作两种不同的基质材料。使用的交联剂是不同浓度和不同持续时间的2,3-丁二酮和甲醛。硫酸链霉素从微球的体外释放具有典型的双相性，先是快速初始释放（“突释效应”），随后是慢得多的释放。载药微球特性的改变会导致释放的第二（慢）阶段发生显著变化。已对不同制剂的释放曲线进行了研究并进行了动力学评估。
