Purpose: Poorly water-soluble drugs when given orally experience limited dissolution due to their low solubility in aqueous solutions. This study aimed to investigate the dissolution enhancement using self-emulsifying drug delivery systems (SEDDS) for Indapamide, a Biopharmaceutical Classification System Type 2 drug. Stability of SEDDS was also assessed.
Methods: Drug containing lipid-based systems that could form SEDDS were prepared with vehicles including Labrafil®M1944CS and Labrasol with or without Capryol™90 or Solutol®HS15. The key quality attributes of SEDDS were determined in terms of size distribution and drug dissolution profiles. Other properties evaluated were critical micelle concentration (CMC), zeta potential and solubility profiles.
Results: SEDDS formed negatively charged dispersions of typically 170-250nm and their CMC were <110mg/L. All SEDDS achieved rapid and significantly higher drug release, which were maintained over 90min when compared to unprocessed drug powder. Dissolution enhancement and size distribution profiles of SEDDS stored at 25 and 40ºC were preserved. Enhancement effect of SEDDS was contributed to formation of stable nano-sized dispersions, high drug solubility in SEDDS and low CMC that withstood dilution by dissolution medium.
Conclusions: Lipid-based systems with Labrasol, Labrafil®M1944CS and Capryol™90 produced SEDDS that led to a significant dissolution enhancement of Indapamide regardless of storage conditions.