Method and system for systemic delivery of growth arresting, lipid-derived bioactive compounds

摘要

A system and method for optimizing the systemic delivery of growth-arresting lipid-derived bioactive drugs or gene therapy agents to an animal or human in need of such agents utilizing nanoscale assembly systems, such as liposomes, resorbable and non-aggregating nanoparticle dispersions, metal or semiconductor nanoparticles, or polymeric materials such as dendrimers or hydrogels, each of which exhibit improved lipid solubility, cell permeability, an increased circulation half life and pharmacokinetic profile with improved tumor or vascular targeting.

主权项

1. A system for delivering a therapeutic compound to an animal or human in need of such system comprising
liposomes that contain a hydrophobic chemotherapeutic agent and/or gene therapy agent, wherein the lipid bilayer of the liposomes comprises cell-permeable pegylated C8 ceramide (PEG-C8) and pegylated distearoylphosphatidylethanolamine (PEG-DSPE) which both stabilize the lipid bilayer and have a molecular weight within the range of 2000-5000 g/mol, wherein the lipid bilayer further comprises a free bioactive ceramide or ceramide analogue such that the free bioactive ceramide or ceramide analogue is independent of being conjugated to polyethylene glycol (PEG) and present at a concentration of at least 30 molar percent.