Itraconazole-Loaded Polycaprolactone Nanoparticle Gel for Enhanced Transdermal Delivery: Development,...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biomedical Engineering

Background:

• Itraconazole (ITZ) is a BCS class II antifungal drug with poor water solubility and variable oral bioavailability, posing formulation challenges.
• Transdermal drug delivery offers an alternative route to overcome oral bioavailability issues and improve therapeutic efficacy.

Purpose of the Study:

• To develop and characterize Polycaprolactone (PCL) nanoparticles for enhanced transdermal delivery of Itraconazole (ITZ).
• To formulate an ITZ-loaded PCL nanoparticle gel for improved skin permeation and sustained drug release.

Main Methods:

• Nanoparticles were prepared using a modified nanoprecipitation method, with the optimized formulation incorporated into a carbopol gel.
• Characterization involved particle size, PDI, zeta potential, encapsulation efficiency (EE), in vitro release, ex vivo permeation, skin irritation, and stability studies.

Main Results:

• The optimized PCL nanoparticles (F2) exhibited favorable characteristics: 154.6 nm size, 0.378 PDI, -10.7 mV zeta potential, and 88.4% EE.
• The gel formulation showed significantly enhanced transdermal permeation (2.32-fold increase) and sustained drug release (80.41-94.34% over 24h) at pH 5.5 and 7.4.
• The formulation was non-irritating and stable for three months, with ITZ confirmed in an amorphous state without interactions.

Conclusions:

• A biocompatible PCL-based gel was successfully developed for enhanced transdermal delivery of Itraconazole.
• The formulation provides sustained drug release and improved skin permeability, representing an effective strategy for ITZ transdermal therapy.