Antimalarial solid self-emulsifying system for oral use: in vitro investigation

摘要

Aim: The low aqueous solubility of artemether and lumefantrine makes them less bioavailable. It is expected that by formulating self-microemulsifying drug-delivery systems (SMEDDS), their aqueous solubility and absorption will thus be enhanced. Results & methodology: Optimized liquid SMEDDS containing artemether and lumefantrine was adsorbed on Neusilin US2? employing spray drying technique to convert it into solid SMEDDS. Almost 90% of both drugs were released within 15 min in their respective official dissolution media. Drug assay and dissolution rate of solid SMEDDS remained unaltered after 3-month storage at 40°C and 75% relative humidity. Conclusion: Reconstitution of solid SMEDDS in water yielded microemulsion with a globule size of 67.74 nm. Complete and faster in vitro release of both drugs from solid SMEDDS was observed as compared with that from marketed tablets.