3.2稳定性尽管SLN与脂肪乳在组成与制备方面极其相似,但SLN不可简单视作“乳滴固化”的胶态脂质分散体系,SLN分散液实质上是一个多相体系,包括胶束、脂质体、过冷熔融液和药物晶体等其他胶体微粒. 存放过程中稳定性差,可能发生粒径增长或药物降解等现象.
3.3突释效应Muhlen等[19]以丁卡因、依托咪酯和泼尼松为模型药物进行的体外药物释放研究显示,以丁卡因、依托咪酯为模型药物制得的SLN,药物在数分钟内即完全释放,且与所选用的类脂种类无关;而以泼尼松为模型药物时,药物先是突释,继而缓慢释放,且可维持释药近1 wk,该体系的释药速率还与类脂的种类关系密切,如选用山榆酸甘油酯为脂质,32 d内仅释药26%,而相同时间内胆固醇体系则释药58%.
4小结与展望
SLN是一种极有发展前景的新型亚微粒给药系统,有多种制备方法,可经多种途径给药,但载药量和稳定性等问题有待解决. 其主要优点是:颗粒粒径小,平均在纳米尺度,可用于注射给药;生理可接受,在制备过程中无有毒残留物;对亲脂性药物有足够的载药能力,通过工艺调整,还可以包封亲水性药物;延长药物释放达数日至数周;通过冷冻干燥或喷雾干燥还可制成固体粉末;通过对其表面进行特征修饰,可实现靶向给药. 我们相信在不久的将来,SLN的制剂可用于临床,造福于患者.
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