SEDEX-Self-Emulsifying Delivery Via Hot Melt Extrusion: A Continuous Pilot-Scale Feasibility Study

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Chemical Engineering

Background:

• Self-emulsifying drug delivery systems (SEDDSs) enhance drug solubility and bioavailability.
• Traditional solidification methods for SEDDSs can be complex and time-consuming.
• Hot melt extrusion (HME) offers a continuous and scalable approach for pharmaceutical formulation.

Purpose of the Study:

• To develop and characterize a continuous pilot-scale solidification process for SEDDSs using HME.
• To evaluate the feasibility of using Soluplus® and Kollidon® VA-64 for SEDDSs solidification via HME.
• To assess the physicochemical properties and self-emulsification performance of the HME-produced extrudates.

Main Methods:

• Oil-binding capacity studies were conducted to determine polymer loading limits.
• Pilot-scale HME was performed using a Coperion ZSK18 extruder with varying SEDDS concentrations (10-30% w/w).
• Extrudates were characterized using differential scanning calorimetry, X-ray scattering, and droplet size analysis after emulsification.

Main Results:

• Polymers demonstrated significant oil-binding capacity, accommodating up to 50% w/w liquid SEDDSs.
• HME processing occurred between 110-160 °C, with observed plasticization effects from the SEDDSs.
• Stable amorphous extrudates were produced, exhibiting self-emulsification in water with mean droplet sizes of 50-300 nm.

Conclusions:

• Continuous pilot-scale HME is a viable and promising alternative for solidifying SEDDSs.
• The developed HME process yields stable amorphous solid dispersions with effective self-emulsification properties.
• This approach offers advantages over traditional solidification techniques for advanced drug delivery applications.