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Cell-Penetrating Peptide-Patchy Deformable Polymeric Nanovehicles with Enhanced Cellular Uptake and Transdermal Delivery.
- Source :
-
Biomacromolecules [Biomacromolecules] 2018 Jul 09; Vol. 19 (7), pp. 2682-2690. Date of Electronic Publication: 2018 Jun 08. - Publication Year :
- 2018
-
Abstract
- 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.
- Subjects :
- Administration, Cutaneous
Adult
Cell Line
Cysteamine chemistry
Female
Humans
Peptide Fragments chemistry
Peptide Fragments pharmacokinetics
tat Gene Products, Human Immunodeficiency Virus chemistry
tat Gene Products, Human Immunodeficiency Virus pharmacokinetics
Glycolipids chemistry
Nanoparticles chemistry
Peptide Fragments administration & dosage
Polyesters chemistry
Skin Absorption
tat Gene Products, Human Immunodeficiency Virus administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1526-4602
- Volume :
- 19
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Biomacromolecules
- Publication Type :
- Academic Journal
- Accession number :
- 29847726
- Full Text :
- https://doi.org/10.1021/acs.biomac.8b00292