Department of Chemical Engineering, National Chung Cheng University, Chia-Yi 62102, Taiwan, ROC.
Colloids Surf B Biointerfaces. 2011 Dec 1;88(2):682-90. doi: 10.1016/j.colsurfb.2011.07.060. Epub 2011 Aug 6.
Solid lipid nanoparticles (SLNs) with complex internal phase were fabricated for formulating stavudine (D4T), delavirdine (DLV), and saquinavir (SQV). The lipids including Compritol 888 ATO, tripalmitin, and cacao butter were stabilized by L-α-phospatidylcholine, cholesteryl hemisuccinate, and taurocholate to form SLNs. The results revealed that the morphology of SLNs was spheroidal with shallow surface pits. An increase in the weight percentage of Compritol 888 ATO increased the average diameter of D4T-entrapping SLNs and decreased that of DLV- and SQV-entrapping SLNs. Preservation at 4°C over 6 weeks slightly enhanced the size of SLNs. For a specific drug, an increase in the entrapment efficiency enlarged the nanocarriers. The order of drug in the average particle diameter and in the entrapment efficiency was SQV>DLV>D4T, in general. In addition, the dissolution of the three drugs from SLNs showed the characteristics of sustained release. The order of drug in the cumulative release percentage was D4T>DLV>SQV. SLNs containing Compritol 888 ATO, tripalmitin, and cacao butter are efficient in carrying antiretroviral agents for medicinal application.
采用复杂内相的固体脂质纳米粒（SLN）来包封司他夫定（D4T）、地拉韦啶（DLV）和沙奎那韦（SQV）。用 L-α-磷脂酰胆碱、胆固醇琥珀酸酯和牛磺胆酸钠稳定包括 Compritol 888 ATO、三棕榈酸甘油酯和可可脂在内的脂质，以形成 SLN。结果表明，SLN 的形态为具有浅表面凹坑的球形。Compritol 888 ATO 的重量百分比增加会增加 D4T 包封 SLN 的平均直径，而降低 DLV 和 SQV 包封 SLN 的平均直径。在 4°C 下保存 6 周会略微增加 SLN 的粒径。对于特定药物，包封效率的增加会增大纳米载体的粒径。总体而言，载药 SLN 的平均粒径和包封效率的药物顺序为 SQV>DLV>D4T。此外，三种药物从 SLN 中的释放表现出持续释放的特征。累积释放百分比的药物顺序为 D4T>DLV>SQV。含有 Compritol 888 ATO、三棕榈酸甘油酯和可可脂的 SLN 是有效的，可用于携带抗逆转录病毒药物进行医疗应用。
