polyethylene glycol-betulinic acid

Polyethylene glycol-betulinic acid (PEG-BA) is a **polymer-drug conjugate** consisting of betulinic acid covalently linked to polyethylene glycol chains. It is designed to address the poor water solubility and low bioavailability of betulinic acid, a naturally occurring pentacyclic triterpene with anticancer activity. Conjugation with polyethylene glycol markedly enhances the drug’s solubility, stability, and pharmacokinetics, resulting in improved tumor selectivity. PEG-BA induces apoptotic cell death in pancreatic cancer (PC) cells by activating both intrinsic (mitochondrial) and extrinsic (death receptor-mediated) pathways, including upregulation of pro-apoptotic genes such as CASPASE 3 and TNF. It displays antioxidant and anti-inflammatory properties, evidenced by decreased IL-6 secretion and enhanced reduction of reactive oxygen species. Experimental studies demonstrate PEG-BA’s increased cytotoxicity and potency against pancreatic cancer cells (MIA PaCa-2) compared to free betulinic acid, with a much lower IC50 and higher selectivity index. This formulation is investigated preclinically for overcoming chemoresistance in solid tumors and may be extendable to other cancers sensitive to betulinic acid polymer conjugates[1][2][3][4][5].

Other names

polyethylene glycol-betulinic acidPEG-BAPEG–BAmultiarm-polyethylene glycol-betulinic acidPEG-betulinic acid conjugate