Highly Branched Betulin Based Polyanhydrides for Self-Assembled Micellar Nanoparticles Formulation

Area of Science:

• Polymer Chemistry
• Materials Science
• Biomedical Engineering

Background:

• Betulin-based polyanhydrides are promising for controlled drug delivery due to their biological activity and low toxicity.
• They can function as polymeric prodrugs or carriers for other active compounds.

Purpose of the Study:

• To synthesize novel amphiphilic branched polyanhydrides using betulin disuccinate (DBB) and a tricarboxylic polyethylene glycol derivative (PEG_COOH).
• To evaluate the anticancer activity and self-assembly properties of these novel branched polyanhydrides.

Main Methods:

• Two-step melt polycondensation of DBB (hydrophobic) and PEG_COOH (hydrophilic) to create copolymers with varying DBB content (10-95 wt%).
• Assessment of copolymer cytostatic activity against cancer cell lines.
• Characterization of self-assembled micelle formation, hydrodynamic diameter, stability, and morphology using scanning electron microscopy.

Main Results:

• Branched polyanhydrides demonstrated higher anticancer activity compared to linear counterparts.
• Polymers self-assembled into spherical micelles in water with hydrodynamic diameters ranging from 144.8 to 561.8 nm.
• Micelle stability was observed over a concentration range of 12.5 µg/mL to 6.8 mg/mL.
• Polymer structure and composition influenced micelle hydrodynamic diameter.

Conclusions:

• Novel branched betulin-based polyanhydrides exhibit significant potential as biodegradable prodrugs or carriers.
• These materials are suitable for developing advanced controlled drug delivery systems.
• The self-assembled micelle characteristics can be tuned by adjusting polymer composition.