Pentafluorophenyl Ester-based Polymersomes as Nanosized Drug-Delivery Vehicles

Area of Science:

• Polymer Chemistry
• Nanotechnology
• Biomaterials Science

Background:

• Polymersomes offer potential as drug delivery systems.
• Biocompatibility and functionalization are key challenges for polymersomes.
• Activated ester chemistry provides a route for polymer modification.

Purpose of the Study:

• To synthesize biocompatible and functionalizable polymersomes using activated ester chemistry.
• To evaluate the encapsulation efficiency and safety of these polymersomes for hydrophilic cargo.
• To assess the in vitro biocompatibility of the polymersomes.

Main Methods:

• Synthesis of precursor polymers via activated ester chemistry (aminolysis).
• Functionalization of polymers using primary amines and a fluorescent dye.
• Characterization of vesicle formation using cryo-transmission electron microscopy (cryoTEM) and light scattering.
• Encapsulation of siRNA using dual centrifugation and assessment by gel electrophoresis.
• In vitro cytotoxicity and protein adsorption studies in human blood serum.

Main Results:

• Successfully synthesized biocompatible and functionalizable polymersomes.
• Achieved high encapsulation efficiencies for hydrophilic cargo like siRNA.
• Demonstrated safe encapsulation of siRNA.
• Exhibited low cytotoxicity in vitro.
• Showed no protein adsorption-induced aggregation in human blood serum.

Conclusions:

• Activated ester chemistry enables the synthesis of versatile, biocompatible polymersomes.
• These polymersomes are promising candidates for nanocarrier-based drug delivery.
• The developed method allows for straightforward functionalization and efficient cargo encapsulation.