Localized delivery of paclitaxel using elastic liposomes: formulation development and evaluation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• The marketed paclitaxel formulation uses Cremophor EL, a solubilizing agent known for toxic side effects.
• There is a need for safer and more effective paclitaxel delivery systems.

Purpose of the Study:

• To develop and characterize an elastic liposomes-based paclitaxel formulation.
• To eliminate the use of Cremophor EL and its associated toxicity.
• To evaluate the efficacy and safety of the new formulation compared to the marketed one.

Main Methods:

• Development and characterization of elastic liposomes loaded with paclitaxel.
• In vitro, ex vivo, and in vivo studies including skin permeation, drug deposition, and hemolytic toxicity assays.
• Fourier Transform Infrared (FTIR) spectroscopy for vesicle-skin interaction analysis.
• Draize test for skin irritation assessment.

Main Results:

• Elastic liposomes successfully loaded paclitaxel at a concentration (6.0 mg/ml) comparable to commercial formulations.
• Demonstrated a 10.8-fold increase in transdermal flux and a 15.0-fold increase in skin drug deposition compared to a simple drug solution.
• Showed significantly reduced hemolysis (11.2% vs. 38%) and no skin irritation in Draize tests.

Conclusions:

• Elastic liposomes represent a promising carrier for paclitaxel, enhancing localized delivery.
• The developed formulation offers improved efficacy and a better safety profile by avoiding Cremophor EL.