Peptide ligand-mediated liposome distribution and targeting to EGFR expressing tumor in vivo

Song, Shuangxi; Liú, Dan; Peng, Jinliang; Sun, Ye; Li, Zonghai; Gu, Jianren; Xu, Yuhong

doi:10.1016/j.ijpharm.2008.07.012

Cited by 162 publications

(99 citation statements)

References 37 publications

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“…95 Epidermal growth factor receptor (EGFR) is an important anti-cancer therapy target that is applicable to many cancer types. 99 Anti-EGFR antibodies and EGF have been conjugated onto liposomes, lipid nanoparticles, chitosan particles and magnetic particles to target cancer cells over-expressing EGFR and the delivery of anticancer drugs or siRNA. In vitro uptake and cytotoxicity of EGF-GemC18-NPs realised with different human breast adenocarcinoma cell lines showed a correlation between EGFR density on the cell surface and cell uptake and toxicity.…”

Section: Lipophilic Prodrugsmentioning

confidence: 99%

Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

2012

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Gemcitabine, an anticancer agent which acts against a wide range of solid tumors, is known to be rapidly deaminated in blood to the inactive metabolite 2',2'-difluorodeoxyuridine and to be rapidly excreted by the urine. Moreover, many cancers develop resistance against this drug, such as loss of transporters and kinases responsible for the first phosphorylation step. To increase its therapeutic levels, gemcitabine is administered at high dose (1000mg/m²) causing sides effects (neutropenia, nausea…).To improve its metabolic stability, its cytotoxic activity and to

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Section: Lipophilic Prodrugsmentioning

confidence: 99%

Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

2012

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“…GE11 is a novel peptide first reported on by Li et al in 2005, 18 and its high affinity for certain EGFR-positive tumor cells has been verified ex vitro and in vivo. 19,20 However, the potential for use of this peptide as a targeting ligand to achieve targeted drug delivery to tumors, especially NSCLC, has not as yet been reported.…”

Section: Introductionmentioning

confidence: 99%

GE11-modified liposomes for non-small cell lung cancer targeting: preparation, ex vitro and in vivo evaluation

Cheng¹,

Huang²,

Liu³

et al. 2014

IJN

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Non-small cell lung cancer (NSCLC) is a serious threat to human health, and 40%–80% of NSCLCs express high levels of epidermal growth factor receptor (EGFR). GE11 is a novel peptide and exhibits high affinity for EGFR binding. The aim of this study was to construct and evaluate GE11-modified liposomes for targeted drug delivery to EGFR-positive NSCLC. Doxorubicin, a broad-spectrum antitumor agent, was chosen as the payload. GE11 was conjugated to the distal end of DSPE-PEG 2000 -Mal by an addition reaction with a conjugation efficiency above 90%. Doxorubicin-loaded liposomes containing GE11 (GE11-LP/DOX) at densities ranging from 0% to 15% were prepared by combination of a thin film hydration method and a post insertion method. Irrespective of GE11 density, the physicochemical properties of these targeted liposomes, including particle size, zeta potential, and drug entrapment efficiency, were nearly identical. Interestingly, the cytotoxic effect of the liposomes on A549 tumor cells was closely related to GE11 density, and liposomes with 10% GE11 had the highest tumor cell killing activity and a 2.6-fold lower half maximal inhibitory concentration than that of the nontargeted counterpart (PEG-LP/DOX). Fluorescence microscopy and flow cytometry analysis revealed that GE11 significantly increased cellular uptake of the liposomes, which could be ascribed to specific EGFR-mediated endocytosis. It was found that multiple endocytic pathways were involved in entry of GE11-LP/DOX into cells, but GE11 assisted in cellular internalization mainly via the clathrin-mediated endocytosis pathway. Importantly, the GE11-modified liposomes showed enhanced accumulation and prolonged retention in tumor tissue, as evidenced by a 2.2-fold stronger mean fluorescence intensity in tumor tissue than the unmodified liposomes at 24 hours. In summary, GE11-modified liposomes may be a promising platform for targeted delivery of chemotherapeutic drugs in NSCLC.

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“…A variety of molecules, including peptides, antibodies, proteins, charged molecules, and some low-molecular weight ligands, such as folate, and nucleic acid-based aptamers, have been studied in conjunction with liposomes for enhanced anticancer treatment. [75][76][77][78] Enhanced tumor targeting can also be attained via exploiting specific features in the tumor microenvironment such as lowered extracellular pH 79) and an altered pattern of extracellular proteins. 80) For example, Zhu et al 80) exploited elevated levels of matrix metalloprotease 2 in the tumor microenvironment to improve cancer cell-specific delivery of loaded drugs via conjugating the anti-nucleosome monoclonal antibody (mAb 2C5) to PEGylated liposomes.…”

Section: Current Applications Of Liposomesmentioning

confidence: 99%

Liposomal Delivery Systems: Design Optimization and Current Applications

Lila

Ishida

2017

Biological & Pharmaceutical Bulletin

287

136

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The liposome, a closed phospholipid bilayered vesicular system, has received considerable attention as a pharmaceutical carrier of great potential over the past 30 years. The ability of liposomes to encapsulate both hydrophilic and hydrophobic drugs, coupled with their biocompatibility and biodegradability, make liposomes attractive vehicles in the field of drug delivery. In addition, great technical advances such as remote drug loading, triggered release liposomes, ligand-targeted liposomes, liposomes containing combinations of drugs, and so on, have led to the widespread use of liposomes in diverse areas as delivery vehicles for anticancer, bio-active molecules, diagnostics, and therapeutic agents. In this review, we summarize design optimization of liposomal systems and invaluable applications of liposomes as effective delivery systems.

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Peptide ligand-mediated liposome distribution and targeting to EGFR expressing tumor in vivo

Cited by 162 publications

References 37 publications

Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

GE11-modified liposomes for non-small cell lung cancer targeting: preparation, ex vitro and in vivo evaluation

Liposomal Delivery Systems: Design Optimization and Current Applications

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