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首页> 外文期刊>Colloids and Surfaces, B. Biointerfaces >Core-matched encapsulation of an oleate prodrug into nanostructured lipid carriers with high drug loading capability to facilitate the oral delivery of docetaxel
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Core-matched encapsulation of an oleate prodrug into nanostructured lipid carriers with high drug loading capability to facilitate the oral delivery of docetaxel

机译：将油酸酯前药核心匹配地封装到具有高载药量的纳米结构脂质载体中，以促进多西他赛的口服给药

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Nanostructured lipid carriers (NLC) have been considered as promising vehicles for oral delivery of taxanes, such as docetaxel (DTX). However, the low drug loading capability (similar to 5%, w/w) has greatly limited their clinical application. In response to this challenge, a novel lipophilic oleate prodrug of DTX (DTX-OA) was synthesized and efficiently encapsulated in NLC using core-match technology, in which liquid lipid (OA) was used as core matrix to enhance compatibility with DTX-OA. DTX-OA-NLC showed uniform particle size of about 100 nm with markedly high drug loading capability (similar to 23% of DTX, w/w) compared with DTX-NLC (similar to 5%, w/w). Besides, DTX-OA-NLC showed better colloidal stability and slower drug release property compared with DTX-NLC. The prepared NLC could be accumulated more easily in MDCK cells than drug solution, and clathrin-mediated endocytosis was the main endocytosis pathway. In situ single-pass intestinal perfusion (SPIP) and intestinal biodistribution studies demonstrated the improved membrane permeability and intestinal wall bioadhesion of NLCs. The bioavailability of DTX-OA-NLC showed 4.04-fold and 2.06-fold higher than DTX solution and DTX-NLC, respectively. These results suggest that the core-matched prodrug-NLC is a promising platform to facilitate the oral delivery of DTX. (C) 2016 Published by Elsevier B.V.
机译：纳米结构脂质载体（NLC）被认为是紫杉烷口服给药的有前途的载体，例如多西紫杉醇（DTX）。但是，低载药量（约5％，w / w）极大地限制了其临床应用。为了应对这一挑战，合成了一种新型的DTX亲脂性油酸酯前药（DTX-OA），并使用核心匹配技术将其有效地包裹在NLC中，其中液体脂质（OA）被用作核心基质以增强与DTX-OA的相容性。与DTX-NLC（约5％，w / w）相比，DTX-OA-NLC显示出约100 nm的均匀粒径，并具有显着高的载药能力（约占DTX的23％，w / w）。此外，与DTX-NLC相比，DTX-OA-NLC具有更好的胶体稳定性和较慢的药物释放性能。制备的NLC比药物溶液更容易在MDCK细胞中积累，而网格蛋白介导的内吞作用是主要的内吞途径。原位单程肠道灌注（SPIP）和肠道生物分布研究表明，NLC的膜通透性和肠壁生物粘附性得到改善。 DTX-OA-NLC的生物利用度分别比DTX溶液和DTX-NLC高4.04倍和2.06倍。这些结果表明，核心匹配的前药-NLC是促进DTX口服递送的有前途的平台。 （C）2016由Elsevier B.V.发布

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