Biodegradable nanoparticles containing doxorubicin-PLGA conjugate for sustained release

Area of Science:

• Biomaterials Science
• Nanotechnology
• Drug Delivery

Background:

• Poly(lactic-co-glycolic acid) [PLGA] is a biodegradable polymer widely used in drug delivery.
• Doxorubicin is a potent chemotherapeutic agent with limitations in its delivery and toxicity profile.

Purpose of the Study:

• To chemically conjugate doxorubicin to PLGA and formulate the conjugate into nanoparticles.
• To achieve sustained release of doxorubicin from the nanoparticles.
• To evaluate the drug loading, release kinetics, and cytotoxicity of the doxorubicin-PLGA nanoparticles.

Main Methods:

• Doxorubicin was conjugated to the terminal end group of PLGA using p-nitrophenyl chloroformate and a primary amine group.
• Nanoparticles (approx. 300 nm) were fabricated using an emulsion-solvent diffusion method.
• Drug release and cytotoxicity (HepG2 cell line) were assessed over time.

Main Results:

• Doxorubicin-PLGA conjugate nanoparticles showed significantly higher loading efficiency (96.6%) and percentage (3.45%) compared to unconjugated doxorubicin.
• Sustained drug release was observed over 25 days for the conjugate, versus rapid release within 5 days for free doxorubicin.
• The released doxorubicin-PLGA oligomer conjugates exhibited comparable cytotoxicity to free doxorubicin in HepG2 cells.

Conclusions:

• Doxorubicin conjugation to PLGA is a viable strategy for developing nanoparticle formulations with high drug loading and sustained release.
• The doxorubicin-PLGA conjugate nanoparticles offer a promising platform for improved chemotherapeutic delivery.
• The conjugate demonstrated slightly reduced cytotoxicity compared to free doxorubicin, suggesting a potentially improved safety profile.