Souto E B, Müller R H
Department of Pharmaceutical Technology, Biotechnology & Quality Management, The Free University of Berlin, Berlin, Germany.
J Microencapsul. 2006 Jun;23(4):377-88. doi: 10.1080/02652040500435295.
Clotrimazole, a fungicidal effective for the local treatment of cutaneous and mucosal infections, was incorporated into solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). The aim was to increase its dermal bioavailability and to control drug release, thereby potentially reducing its side effects. Prior to the release studies, the carrier was optimized and characterized by using different techniques. Laser diffractometry (LD), photon correlation spectroscopy (PCS) and scanning electron microscopy (SEM) indicated that SLN were spherical in shape with a mean size of approximately 400 nm. Some aggregation phenomena occurred during preparation of SEM samples due to the lipid character of the carriers. No physico-chemical instability of the drug-loaded lipid nanoparticles was detected during 2 years of storage at different temperatures. X-ray and DSC results suggested that during storage time the drug remained molecularly dispersed in the lipid matrix. Drug associated to SLN and NLC in its crystal form could be excluded.
克霉唑是一种对皮肤和黏膜感染局部治疗有效的杀菌剂,被载入固体脂质纳米粒(SLN)和纳米结构脂质载体(NLC)中。目的是提高其皮肤生物利用度并控制药物释放,从而有可能降低其副作用。在进行释放研究之前,通过使用不同技术对载体进行了优化和表征。激光衍射法(LD)、光子相关光谱法(PCS)和扫描电子显微镜(SEM)表明,SLN呈球形,平均尺寸约为400nm。由于载体的脂质特性,在制备SEM样品过程中出现了一些聚集现象。在不同温度下储存2年期间,未检测到载药脂质纳米粒的物理化学不稳定性。X射线和差示扫描量热法(DSC)结果表明,在储存期间药物仍以分子形式分散在脂质基质中。可以排除以晶体形式与SLN和NLC结合的药物。