TUMOR TARGETED LIPOSOMAL DRUG DELIVERY SYSTEM

摘要

The conventional chemotherapy and radiotherapy treatments are known to cause systemic side effects, therefore current research in the field focuses on targeted therapies specifically to tumor sites. Liposomes offer several advantages in this context, mainly being biodegradable and non-toxic carriers for especially hydrophobic drugs that have very limited bioavailability when administered orally. The present invention is related to a liposomal drug delivery system that is loaded with Cycloocygenase-2 (COX- 2) inhibitors, is surface grafted by Poly-ethylene glycol (PEG) chains and is targeted to cells overexpressing EGFR. The invention aims to inhibit both pro-inflammatory COX-2 pathway and EGFR pathway simultaneously, therefore obtain a synergistic effect in terms of anti-tumor efficacy. A specific example for a liposomal delivery system in accordance with the invention is composed of DSPC and cholesterol, loaded with Celecoxib, surface grafted with PEG(2000)- DSPE and a covalently bound anti-EGFR MAb molecules to Maleimide functionalized PEG(2000)-DSPE chains.