Design of self-microemulsifying drug delivery systems using a high-throughput formulation screening system

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Formulation Development

Background:

• Self-microemulsifying drug delivery systems (SMEDDS) enhance the bioavailability of poorly soluble drugs.
• Efficient formulation screening is crucial for developing effective SMEDDS.

Purpose of the Study:

• To evaluate the applicability of a previously developed high-throughput formulation screening (HTFS) system for designing SMEDDS.
• To demonstrate the efficiency of the HTFS system in selecting optimal SMEDDS components.

Main Methods:

• Utilized a poorly soluble drug (Nilvadipine), oil (Sefsol-218), hydrophilic surfactants (HS), and lipophilic surfactants (LS).
• Employed the HTFS system to screen 2455 formulations and select SMEDDS.
• Identified optimal HS (HCO60) and LS (Plurol OLEIQUE CC497) based on screening data.
• Optimized formulations were selected based on minimum turbidity and microemulsion characteristics.

Main Results:

• The HTFS system successfully selected SMEDDS formulations from 2455 candidates.
• HCO60 and Plurol OLEIQUE CC497 were identified as superior emulsifying agents.
• Five optimized SMEDDS formulations were developed, producing fine microemulsions (<33.6 nm) without phase separation or drug precipitation.
• The screening process achieved a high throughput of 400 formulations/person/day for 600 mg drug batches.

Conclusions:

• The HTFS system provides a rapid and efficient method for designing SMEDDS formulations.
• This approach accelerates the development of effective drug delivery systems.