Cell-Penetrating Peptide-Patchy Deformable Polymeric Nanovehicles with Enhanced Cellular Uptake and Transdermal Delivery,Biomacromolecules

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Cell-Penetrating Peptide-Patchy Deformable Polymeric Nanovehicles with Enhanced Cellular Uptake and Transdermal Delivery
Biomacromolecules ( IF 5.5 ) Pub Date : 2018-05-30 00:00:00 , DOI: 10.1021/acs.biomac.8b00292
Daehwan Park ₁ , Jin Yong Lee ₁ , Heui Kyoung Cho ₂ , Woo Jin Hong ₂ , Jisun Kim ₃ , Hyemyung Seo ₃ , Ikjang Choi ₁ , Youngbok Lee _{1,

4} , Juhyeon Kim _{5,

6} , Sun-Joon Min ₄ , So-Hyun Yoon ₇ , Jae Sung Hwang ₇ , Kwang Jin Cho ₈ , Jin Woong Kim _{1,

4}

Affiliation

We herein propose a polymeric nanovehicle system that has the ability to remarkably improve cellular uptake and transdermal delivery. Cell-penetrating peptide-patchy deformable polymeric nanovehicles were fabricated by tailored coassembly of amphiphilic poly(ethylene oxide)-block-poly(ε-caprolactone) (PEO-b-PCL), mannosylerythritol lipid (MEL), and YGRKKRRQRRR-cysteamine (TAT)-linked MEL. Using X-ray diffraction, differential scanning calorimetry, and nuclear magnetic resonance analyses, we revealed that the incorporation of MEL having an asymmetric alkyl chain configuration was responsible for the deformable phase property of the vehicles. We also discovered that the nanovehicles were mutually attracted, exhibiting a gel-like fluid characteristic due to the dipole–dipole interaction between the hydroxyl group of MEL and the methoxy group of PEO-b-PCL. Coassembly of TAT-linked MEL with the deformable nanovehicles significantly enhanced cellular uptake due to macropinocytosis and caveolae-/lipid raft-mediated endocytosis. Furthermore, the in vivo skin penetration test revealed that our TAT-patchy deformable nanovehicles remarkably improved transdermal delivery efficiency.

中文翻译：

具有细胞吸收和透皮递送的细胞穿透性肽斑片状可变形聚合物纳米车辆。

我们在本文中提出了一种聚合物纳米载体系统，其具有显着改善细胞摄取和透皮递送的能力。-细胞穿透肽-片状变形聚合纳米载体被定制coassembly的两亲性聚（环氧乙烷）制造嵌段-聚（ε -己内酯）（PEO- b-PCL），甘露糖基赤藓糖醇脂质（MEL）和YGRKKRRQRRR-半胱胺（TAT）连接的MEL。使用X射线衍射，差示扫描量热法和核磁共振分析，我们发现掺入具有不对称烷基链构型的MEL负责车辆的可变形相性质。我们还发现，由于MEL的羟基和PEO - b -PCL的甲氧基之间的偶极-偶极相互作用，纳米车辆相互吸引，表现出凝胶状的流体特性。TAT连接的MEL与可变形的纳米载体的共组装显着增强了细胞的摄取，这是由于巨胞饮作用和小窝/脂质筏介导的内吞作用。此外，体内皮肤渗透测试表明，我们的TAT补丁可变形纳米车辆显着提高了透皮递送效率。

更新日期：2018-05-30

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