Optimized aptamer functionalization for enhanced anticancer efficiency in vivo.

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Drug Delivery

Background:

• Nucleic acid aptamers (Apt) are key for targeted cancer diagnosis and treatment.
• Incorporating Apt into nanocarriers is crucial for effective drug delivery.
• Current Apt incorporation methods lack comparative performance data, hindering clinical translation.

Purpose of the Study:

• To investigate the impact of different Apt incorporation strategies on nanocarrier properties and anti-tumor efficacy.
• To compare covalent conjugation versus electrostatic interactions for Apt functionalization of polymeric prodrugs.
• To elucidate how Apt incorporation affects in vivo performance for liver cancer treatment.

Main Methods:

• Fabricated two types of Apt-functionalized polymeric prodrugs: Apt/CS-FU (covalent) and Apt-CS-FU (electrostatic).
• Assessed in vitro and in vivo anti-tumor efficacy and targeting properties.
• Compared nanocarrier size, serum stability, and circulation time.

Main Results:

• Both Apt/CS-FU and Apt-CS-FU showed similar in vitro targeting and anti-tumor efficiency.
• Apt-CS-FU demonstrated a 1.5-fold higher tumor inhibition rate in murine models compared to Apt/CS-FU.
• Apt-CS-FU exhibited smaller size and prolonged in vivo circulation in serum.

Conclusions:

• The strategy for incorporating aptamers significantly influences nanocarrier performance.
• Covalent conjugation of Apt (Apt-CS-FU) enhances in vivo anti-tumor efficacy through improved pharmacokinetics.
• Findings provide insights for rational design of Apt-functionalized nanoplatforms for improved cancer therapy.