Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin.
Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin.
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二氧化硅包被的柔性脂质体作为纳米混合递送系统，用于增强姜黄素的口服生物利用度
DOI：
10.2147/ijn.s38043
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发表时间：
2012
影响因子：
8
通讯作者：
Chen Z
中科院分区：
文献类型：
--
作者：
Li C;Zhang Y;Su T;Feng L;Long Y;Chen Z
我们研究了柔性脂质体作为一种潜在的口服给药系统。然而，当面对胃肠道的恶劣环境时，增强的膜流动性和结构变形性可能需要脂质体表面修饰。本研究以姜黄素为模型药物，采用薄膜法均质化制备了硅胶包覆的柔性脂质体（CUR-SLs），并通过溶胶-凝胶法制备了硅胶壳层。我们系统地研究了CUR-SL的物理性质、药物释放行为、药效学和生物利用度。CUR-SL的平均粒径为157 nm，多分散指数为0.14，表观包封率为90.62%。体外释放实验表明，与无硅胶包被的姜黄素柔性脂质体（CUR-FL）相比，CUR-SL对人工胃液的稳定性明显提高，在人工肠液中的释药更加持久。CUR-SL和CUR-FL的生物利用度分别是姜黄素混悬液的7.76倍和2.35倍。二氧化硅包覆显著提高了柔性脂质体的稳定性，与CUR-FL相比，CUR-SL的生物利用度提高了3.31倍，表明二氧化硅包覆的柔性脂质体可以作为潜在的载体，通过口服途径递送水溶性差的药物，并提高生物利用度。
We investigated flexible liposomes as a potential oral drug delivery system. However, enhanced membrane fluidity and structural deformability may necessitate liposomal surface modification when facing the harsh environment of the gastrointestinal tract. In the present study, silica-coated flexible liposomes loaded with curcumin (CUR-SLs) having poor water solubility as a model drug were prepared by a thin-film method with homogenization, followed by the formation of a silica shell by the sol-gel process. We systematically investigated the physical properties, drug release behavior, pharmacodynamics, and bioavailability of CUR-SLs. CUR-SLs had a mean diameter of 157 nm and a polydispersity index of 0.14, while the apparent entrapment efficiency was 90.62%. Compared with curcumin-loaded flexible liposomes (CUR-FLs) without silica-coatings, CUR-SLs had significantly higher stability against artificial gastric fluid and showed more sustained drug release in artificial intestinal fluid as determined by in vitro release assays. The bioavailability of CUR-SLs and CUR-FLs was 7.76- and 2.35-fold higher, respectively, than that of curcumin suspensions. Silica coating markedly improved the stability of flexible liposomes, and CUR-SLs exhibited a 3.31-fold increase in bioavailability compared with CUR-FLs, indicating that silica-coated flexible liposomes may be employed as a potential carrier to deliver drugs with poor water solubility via the oral route with improved bioavailability.