Doxorubicin-Loaded Poly(Substituted Glycolide)-Based Nanoparticles for Long-Term Storage

Area of Science:

• Polymer chemistry
• Nanotechnology
• Pharmaceutical sciences

Background:

• Polymeric nanoparticles (PNP) are crucial for drug delivery.
• Preventing nanoparticle agglomeration during storage is essential for maintaining efficacy.
• Doxorubicin (DOX)-loaded nanoparticles require stable formulations for long-term use.

Purpose of the Study:

• To investigate optimal conditions for maintaining the size of doxorubicin (DOX)-loaded poly-(diisobutyl glycolide) (PDIBG) and poly-(diisopropyl glycolide) (PDIPG) nanoparticles (NP) during long-term storage.
• To evaluate the impact of lyophilization on the stability of DOX-loaded PDIBG and PDIPG NPs.
• To determine effective cryoprotectants for stabilizing lyophilized nanoparticles.

Main Methods:

• Synthesis of PDIBG and PDIPG homopolymers.
• Production of DOX-loaded NPs using single-emulsion solvent evaporation.
• Optimization of nanoparticle formulations for size and encapsulation efficiency.
• Lyophilization of NPs at different concentrations and freezing temperatures (-20 and -50 °C).
• Assessment of nanoparticle size and PDI after storage at 4 °C and -20 °C for 2 months, with and without cryoprotectants (glucose and sucrose).

Main Results:

• Optimal DOX-loaded PDIBG NPs: 253 ± 7 nm size, 0.06 ± 0.02 PDI, 58.3% EE.
• Optimal DOX-loaded PDIPG NPs: 253 ± 7 nm size, 0.08 ± 0.04 PDI, 73.9% EE.
• Lyophilization with 5% or 10% glucose and sucrose enabled stable storage of DOX-loaded PDIBG and PDIPG NPs for 2 months at 4 °C and -20 °C.
• Maintained particle size and PDI values were observed in the presence of cryoprotectants.

Conclusions:

• Lyophilization is an effective method for stabilizing DOX-loaded PDIBG and PDIPG nanoparticles.
• Glucose and sucrose act as effective cryoprotectants, preventing agglomeration and maintaining nanoparticle integrity during storage.
• Stable storage conditions were established for drug-loaded polymeric nanoparticles, enhancing their potential for pharmaceutical applications.