Liposome for blocking site-specifically chemokine-related inflammatory processes in vascular diseases and metastasis

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent discloses a targeted drug delivery system using nanocarriers—specifically liposomes and polymeric nanoparticles—that are engineered to deliver chemokine antagonists or chemokine receptor antagonists directly to inflamed vascular tissue or metastatic sites. The nanocarriers are surface-modified with antibodies or peptides that specifically recognize VCAM-1, a molecule expressed on activated endothelial cells in inflamed or metastatic regions. Upon binding to the VCAM-1 on endothelial cells, the nanocarriers release their drug payload locally, thereby inhibiting leukocyte migration in vascular inflammation (such as atherosclerosis) or the spread of cancer cells (metastasis). This method increases drug concentration at disease sites and minimizes side effects elsewhere in the body.

Use CasesContent extracted from patent full text and abstract with AI.

• Targeted treatment of atherosclerosis by inhibiting inflammatory leukocyte migration into vascular plaques.
• Blocking cancer metastasis by preventing tumor cell migration through the vasculature.
• Site-specific delivery of chemokine antagonists or receptor antagonists to areas of vascular inflammation or cancerous metastasis.
• Reducing systemic side effects for drugs used in chronic inflammatory diseases or cancer therapy.
• Use as a research tool in drug delivery and inflammation/metastasis models.

BenefitsContent extracted from patent full text and abstract with AI.

• Provides targeted delivery of drugs to disease sites, maximizing local therapeutic effect while limiting systemic exposure.
• Reduces risk of side effects common with systemic inhibition of chemokines or their receptors, such as immunosuppression.
• Increases the stability and circulation time of therapeutic agents in blood via surface PEGylation and optimized nanoparticle/liposome design.
• Demonstrated effectiveness in inhibiting both atherosclerotic progression and cancer metastasis in animal models.
• Utilizes endogenous disease markers (VCAM-1) for highly specific targeting of inflamed or metastatic tissues.

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Inventors & Applicants

Patent Abstract

The invention provides a method for blocking site-specifically chemokine-related inflammatory processes in vascular diseases and metastasis employing vascular targeted nanocarrier. In particular, the present invention provides two types of targeted n ano c arrier (NC) with encapsulated c hemokine a ntagonists (CA) or c hemokine r eceptor a ntagonists (CRA): stabilised t arget-sensitive l iposomes (TSL) and p olymeric n anoparticles (PNP). Both types of nanocarrier have attached on their surface monoclonal antibodies or peptides that recognize VCAM-1 expressed on activated endothelial cells (EC). After binding of the nanocarrier to the VCAM-1 expressed on EC, the encapsulated CA or CRA are released and will block the interaction between chemokine and chemokine receptors. This will lead to an inhibition of transmigration of leukocytes (in atherosclerosis) or of tumor metastatic cells (in cancer). The invention provides a carrier system which delivers effective concentrations of drugs specifically to the diseased (target) sites and reduces the drug concentrations at non-target sites. This results in a reduced, even absent, occurrence of side effects. The nanocarriers described in this invention have the potential to function as long-lasting vehicles for delivering selectively CA or CRA to activated endothelium.