Formulation and Evaluation of Morin-Loaded Solid Lipid Nanoparticles
Formulation and Evaluation of Morin-Loaded Solid Lipid Nanoparticles
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DOI：
10.1248/bpb.b16-00300
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发表时间：
2016-09-01
影响因子：
2
通讯作者：
Onishi, Hiraku
中科院分区：
文献类型：
--
作者：
Ikeuchi-Takahashi, Yuri;Ishihara, Chizuko;Onishi, Hiraku
在这项研究中，固体脂质纳米粒（SLN）的悬浮液制备使用的基础上，或没有乙基纤维素（EC）和聚乙烯醇（PVA）和聚山梨醇酯（吐温）60表面活性剂的硬脂肪。市售PVA的皂化度和聚合度各不相同，并且研究了在具有或不具有EC的情况下从硬脂肪形成SLN的适当PVA。一个相对低的皂化度的PVA需要可重复地形成SLN悬浮液没有EC和相对高的皂化度的PVA是合适的SLN与EC。桑色素在有EC的SLN中的释放比无EC的SLN更持久。含EC和不含EC的前哨淋巴结的最大血浆浓度（C-max）几乎相同，且均高于桑色素悬液的最大血浆浓度（C-max）。与桑色素混悬液和不含EC的SLN相比，含EC的SLN 0 - 360 min的曲线下面积（AUC（0-360））增加。与其他配方相比，EC和非常低的皂化度PVA的SLN的中值直径降低，并且桑色素释放对于该配方更持续。具有EC和极低皂化度PVA的SLN显示出比具有EC但不具有极低皂化度PVA的SLN更高的C-max和AUC（0-360）。优化的SLN与EC和一个非常低的皂化度的PVA通过增加可访问性的肠上皮细胞表面的粒径减小和增加的渗透SLN封装桑色素通过肠膜的持续释放性能，提高生物利用度。
In this study, solid lipid nanoparticle (SLN) suspensions were prepared using a base of hard fat with or without ethylcellulose (EC) and polyvinyl alcohols (PVA) and polysorbate (Tween) 60 surfactants. Commercially available PVAs vary in their degree of saponification and polymerization, and the appropriate PVAs to form SLNs from hard fat with or without EC were investigated. A relatively low-saponification-degree PVA was required to reproducibly form SLN suspensions without EC and relatively high-saponification-degree PVAs were suitable for SLNs with EC. The release of morin from SLNs with EC was more sustained than that from SLNs without EC. The maximum plasma concentration (C-max) of SLNs with and without EC were almost the same, and both were higher than that of a morin suspension. The area under the curve for 0 to 360 min (AUC(0-360)) of SLNs with EC was increased compared with those of a morin suspension and SLNs without EC. The median diameter of SLNs with EC and a very low-saponification-degree PVA was decreased compared to other formulation, and morin release was more sustained for this formulation. SLNs with EC and a very low-saponification-degree PVA showed higher C-max and AUC(0-360) than SLNs with EC lacking a very low-saponification-degree PVA. The optimized SLNs with EC and a very low-saponification-degree PVA improved bioavailability via increased accessibility to the enterocyte surface by decreased particle size and increased permeation of SLN encapsulated morin through the intestinal membrane by sustained release properties.