Characterisation and evaluation of self-microemulsifying drug delivery system of brucea javanica oil

A self-microemulsifying drug delivery system (SMEDDS) of Brucea javanica oil (BJO) was developed and evaluated for its oral absorption and bioavailability. Based on a solubility study and pseudo-ternary phase diagrams, the self-microemulsifying formulation composed of BJO, Cremorphor RH40, Plurol Oleique CC 497 and glycerol (30/42/20/8, % w/w) was prepared and characterised, including particle size, morphology, in vitro cytotoxicity and in vivo anti-tumour effects. The mean diameter of the final formulation was 41.5±3.5±nm. The BJO-loaded SMEDDS (BJOS) and the control preparation of BJO were administered orally to beagle dogs for pharmacokinetics and bioavailability studies. Oleic acid, which was considered as the main active and indicative component in BJO, was determined by gas chromatography. The cytotoxicity and anti-tumour effects of BJOS were evaluated in SMMC-7721 and BGC-823 cancer cell lines and sarcoma 180-bearing mice. The data showed that the oral relative bioavailability of commercial emulsion of BJO (BJOE) was 2.3-fold higher than that of BJO. Moreover, the IC₅₀ value of BJOS group was nearly one-fourth compared to that of commercial BJOE. BJOS could significantly inhibit tumour growth via intra-gastric administration. The Letter illustrates that the developed SMEDDS formulation possessed great potential to be an alternative for traditional oral formulations of BJO.