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Targeting of liposomes via PSGL1 for enhanced tumor accumulation.

ABSTRACT:

Purpose

To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium.

Methods

PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel streptavidin-protein G linker molecule. Loading of PSGL1 liposomes with luciferin allowed their binding to e-selectin and activated HUVEC to be quantified in vitro and their stability, pharmacokinetics and tumor accumulation to be tested in vivo using murine models.

Results

PSGL1 liposomes showed 5-fold (p?7-fold (p?3-fold enhancement in the level of delivery to tumors (p?ConclusionsThe technologies and strategies described here may contribute to clinical improvements in the selectivity and efficacy of liposomal drug delivery agents.

SUBMITTER: Carlisle R

PROVIDER: S-EPMC3553414 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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Targeting of liposomes via PSGL1 for enhanced tumor accumulation.

Carlisle Robert R Seymour Leonard W LW Coussios Constantin C CC

Pharmaceutical research 20120920 2

<h4>Purpose</h4>To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium.<h4>Methods</h4>PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel streptavidin-protein G linker molecule. Loading of PSGL1 liposomes with luciferin allowed their binding to e-selectin and activated HUVEC to be quantified in vitro and ...[more]

PMID: 22992830

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