Improved Drug Delivery through Amide-Functionalized Polycaprolactones: Enhanced Loading Capacity and Sustained Drug...

Area of Science:

• Polymer Chemistry
• Materials Science
• Nanotechnology

Background:

• Polymeric micelles are promising drug delivery vehicles.
• Challenges include instability, low drug loading capacity (DLC), and premature drug leakage.

Purpose of the Study:

• To develop enhanced polymeric micelles with improved properties.
• To investigate disubstituted γ-amide functionalized ε-caprolactone (ε-CL) monomers for micelle formation.
• To evaluate drug loading, release, and in vitro efficacy.

Main Methods:

• Synthesis of three hydrophobic ε-CL monomers with varying substituents.
• Ring-opening polymerization using poly(ethylene glycol) (PEG) as a hydrophilic block.
• Self-assembly into micelles and doxorubicin (DOX) loading.
• In vitro drug release studies and cell viability assays.

Main Results:

• Disubstituted monomers doubled substituent density, enhancing micelle properties.
• PEG-b-poly(N-propyl-N-benzyl-7-oxopane-4-carboxamide) (PEG-b-PBnPyCL) micelles achieved 7.33 wt % DLC.
• pH-responsive DOX release was observed in acidic conditions.
• DOX-loaded PEG-b-PBnPyCL micelles showed ~20% viability in MDA-MB-231 cancer cells.

Conclusions:

• Disubstituted amide functionalized ε-CL monomers significantly improve polymeric micelle performance.
• These enhanced micelles demonstrate potential for advanced drug delivery with clinical translation possibilities.