摘要
探索一种表面修饰二氧化硅的含醇脂质体(硅-醇质体)作为姜黄素口服给药载体的可行性。采用乙醇注入法制备姜黄素含醇脂质体,经四乙氧基硅烷(TEOS)溶胶凝胶反应于醇质体表面形成二氧化硅层,制得姜黄素硅-醇质体,考察其理化性状及体外释放特性,并进行正常大鼠口服给药的药动学评价。所得载姜黄素的硅-醇质体平均粒径为(478.5±80.3)nm,多分散系数为0.285±0.042,其表观包封率均值为80.77%。与姜黄素醇质体的易沉淀﹑难释放比较,姜黄素硅-醇质体初步表现为在近人工胃液条件下结构稳定,在近人工肠液条件下稳步释放。与姜黄素混悬剂及醇质体相比,姜黄素硅-醇质体口服给药的相对生物利用度分别为1 185.53%和225.56%。醇质体表面经二氧化硅修饰后其稳定性得到显著提高,并可促进其包载的姜黄素经口服吸收,为口服给药尤其是中药口服纳米制剂研究提供了新思路。
The aim of this study is to investigate the feasibility of silica-coated ethosome as a novel oral delivery system for the poorly water-soluble curcumin （as a model drug）. The silica-coated ethosomes loading curcumin （CU-SE） were prepared by alcohol injection method with homogenization, followed by the precipitation of silica by sol-gel process. The physical and chemical features of CU-SEs, and curcumin release were determined in vitro. The pharmacodynamics and bioavailability measurements were sequentially performed. The mean diameter of CU-SE was （478.5 ~ 80.3） nm and the polydispersity index was 0.285 ~ 0.042, while the mean value of apparent drug entrapment efficiency was 80.77%. In vitro assays demonstrated that CU-SEs were significantly stable with improved release properties when compared with curcumin-loaded ethosomes （CU-ETs） without silica-coatings. The bioavailability of CU-SEs and CU-ETs was 11.86- and 5.25- fold higher, respectively, than that of curcumin suspensions （CU-SUs） in in vivo assays. The silica coatings significantly promoted the stability of ethosomes and CU-SEs exhibited 2.26-fold increase in bioavailablity relative to CU-ETs, indicating that the silica-coated ethosomes might be a potential approach for oral delivery of poorly water-soluble drugs especially the active ingredients of traditional Chinese medicine with improved bioavailability.
出处
《药学学报》
CAS
CSCD
北大核心
2012年第11期1541-1547,共7页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(81102404)
国家重大新药创制资助项目(2010ZX09401-306-1-4)
重庆市自然科学基金资助项目(cstc2011jjA1585)
重庆市高等学校青年骨干教师资助计划
