Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 111, Issue 6, Pages 1719-1727Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2021.11.022
Keywords
Liposomes; Octaarginine (R-8); PEG; Cell-penetrating peptide; Active targeting; Glioma
Funding
- Egypt-Japan partnership scholarship by the Ministry of Higher Education of the Arab Republic of Egypt [CAM-751-FM-06-01]
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This study developed novel octaarginine (R-8) peptide-HFQ lipid grafted PEGylated liposomes for glioma cells targeting. The results showed that these liposomes exhibited excellent in vitro cellular association and intracellular distribution properties, suggesting their potential as a drug delivery system for tumor targeting.
The use of peptide ligand modified PEGylated liposomes has been widely investigated for tumor targeting. Peptides are mainly inserted in the liposomal lipid bilayer using PEG(2K)-lipid spacer (Peptide-PEG(2K)-DSPE). However, a lower cellular uptake from longer nonlinear PEG(2K) spacer was reported, we here synthesized a high functionality and quality (HFQ) lipid with a short, linear serine-glycine repeated peptide [(SG)(5)] spacer. The objective of the current study is to develop novel octaarginine (R-8) peptide-HFQ lipid grafted PEGylated liposomes for glioma cells targeting. In vitro liposomes characterization showed that the mean particle size of all liposomal formulations was in the nano-scale range < 120 nm, with a small PDI value (i.e. similar to 0.2) and had a spherical shape under Transmission Electron Microscope, indicating a homogenous particle size distribution. The flow cytometry in vitro cellular association data with U251 MG and U87 cells revealed that 1.5% R-8-(SG)(5)-lipid-PEGylated liposomes exhibited significantly higher cellular association of similar to 15.87 and 7.59-fold than the conventional R-8-PEG(2K)-lipid-PEGylated liposomes (10.4 and 6.19-fold), respectively, relative to the unmodified PEGylated liposomes. Moreover, intracellular distribution studies using confocal laser scanning microscopy (CLSM) corroborated the results of the in vitro cell association. The use of ligand-HFQ-lipid liposomes could be a potential alternative to ligand-PEG(2K)-lipid-modified liposomes as a drug delivery system for tumor targeting. (C) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
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