Self-emulsifying Pellets Prepared by Extrusion/Spheronization: In vitro/In vivo Evaluation

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Self-emulsifying drug delivery systems (SEDDS) are gaining traction for improving oral bioavailability of lipophilic drugs.
• Liquid lipid formulations can present challenges in handling and manufacturing.
• Patented SEDDS formulations guided the selection of drugs and excipients.

Purpose of the Study:

• To assess the feasibility of producing solid self-emulsifying pellets via extrusion/spheronization.
• To enhance the bioavailability of a selected drug.
• To address limitations associated with liquid lipid-based formulations.

Main Methods:

• Preparation of pellets using liquid self-nanoemulsifying drug delivery systems (SNEDDS) with specific oil, surfactant, and co-surfactant ratios.
• Incorporation of adsorbent (silicon dioxide), microcrystalline cellulose, pregelatinized starch, croscarmelose sodium, and corn starch.
• Utilizing the extrusion/spheronization technique for pellet formation.

Main Results:

• Solid pellets containing approximately 32% liquid SNEDDS were produced with uniform size and spherical shape.
• Post-self-emulsification droplet sizes were comparable to the initial liquid SNEDDS (26.5 nm vs. 24.8 nm).
• In vitro drug release was significantly higher than the plain drug, with a 5-fold increase in AUC0-36h for sertraline compared to the plain drug.

Conclusions:

• Extrusion/spheronization is a viable method for producing spherical, self-emulsifying pellets with low friability.
• These pellets effectively transfer lipophilic compounds into the aqueous phase.
• The developed pellets demonstrate significant potential for enhancing oral absorption of lipophilic drugs.