Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Liquid formulations of bile salt/phospholipid mixed micelles (MMs) face limitations for oral drug delivery.
• Poorly water-soluble drugs require advanced delivery systems to improve oral absorption.

Purpose of the Study:

• To evaluate the feasibility of preparing bile salt/phospholipid MM precursor (preMM) pellets using fluid-bed coating technology.
• To enhance the oral bioavailability of fenofibrate (FB), a model poorly soluble drug.

Main Methods:

• Fenofibrate (FB) and sodium deoxycholate (SDC)/phospholipids (4:6 ratio) were used to form MMs.
• Polyethylene glycol (PEG) 6000 served as a dispersion matrix for MM precipitation onto pellets via fluid-bed coating.
• PreMM pellets were characterized for reconstitution, redispersion, and in vivo bioavailability.

Main Results:

• Fluid-bed coating efficiently produced spherical and intact preMM pellets.
• Reconstituted MMs from preMM pellets showed superior redispersion compared to solid dispersion pellets and Lipanthyl®.
• PreMM pellets (FB:PEG:micellar carrier 1:1.5:1.5) achieved 284% and 145% bioavailability versus Lipanthyl® and solid dispersion pellets, respectively.

Conclusions:

• Fluid-bed coating is a viable technology for producing preMM pellets with enhanced oral bioavailability.
• This approach offers significant potential for improving the delivery of poorly water-soluble drugs.