Orally delivered salmon calcitonin-loaded solid lipid nanoparticles prepared by micelle-double emulsion method via the combined use of different solid lipids
Orally delivered salmon calcitonin-loaded solid lipid nanoparticles prepared by micelle-double emulsion method via the combined use of different solid lipids
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不同固体脂质联合胶束双乳化法制备口服鲑鱼降钙素固体脂质纳米粒
DOI：
10.2217/nnm.12.141
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发表时间：
2013-07-01
期刊：
影响因子：
5.5
通讯作者：
Huang, Yuan
中科院分区：
文献类型：
--
作者：
Chen, Chunhui;Fan, Tingting;Huang, Yuan
本研究的目的是开发一种新的口服纳米微粒系统，以提高鲑鱼降钙素（sCT）的生物利用度。材料和方法：采用胶束复乳法，分别以硬脂酸（SA）和三硬脂酸甘油酯（TP、trimyristin、trilaurin）为原料，制备了4种sCT固体脂质纳米粒（SLN）。结果如下：与其他SLN相比，SA和TP联合应用不仅能显著改善SLN的胶体稳定性，提高药物在模拟肠液中的稳定性，而且能显著增加SLN对药物的细胞内摄取（p < 0.05）。内化的机制是一个主动运输参与网格蛋白和小窝依赖的内吞作用。在体内，用SA和TP制备的sCT SLN表现出最高的血浆Ca 2+水平降低（17.44 +/- 3.68%），生物利用度为13.01 +/-3.24%。结论：SA和TP作为固体脂质形成的SLN可能是一种很有前途的多肽类药物口服给药载体。
The purpose of this study was to develop a new orally delivered nanoparticulate system to improve the bioavailability of salmon calcitonin (sCT). Materials & methods: Four sCT-loaded solid lipid nanoparticles (SLNs) were prepared successfully by micelle-double emulsion technique via either the sole use of stearic acid (SA) or the combined use of SA and triglycerides (including tripalmitin [TP], trimyristin or trilaurin). Results: Compared with other SLNs, the combination of SA and TP could not only significantly improve the colloidal stability of SLNs and enhance the drug stability in the simulated intestinal fluids, but also intensively increase the intracellular uptake of drugs compared with the other SLNs (p < 0.05). The mechanism of internalization was an active transport involved in clathrin-and caveolae-dependent endocytosis. In vivo, the sCT SLNs prepared with SA and TP exhibited the highest reduction of plasma Ca2+ level (17.44 +/- 3.68%) with a bioavailability of 13.01 +/- 3.24%. Conclusion: The SLNs formed by SA and TP as the solid lipids may be a promising carrier for oral delivery of peptide drugs.