AIM: To prepare the self
emulsification nano-microemulsion of paclitaxel and investigate its
hypersensitivity in guinea pig
with simultaneous pharmcokinetic process of nano-microemulsion in rats. METHODS:The criteria of paclitaxel microemulsion formation were studied with triangle phase diagram and the preparation of self microemulsion had been optimized by uniform design. Comparing with paclitaxel injection in
hypersensitivity and pharmacokinetic parametes of self microemulsion in rats were also carried out. RESULTS: Stable concentration of microemulsion was made up of tricaprylin∶tributyrin 1∶1 as oil phase, dehydrated ethanol as assistent emulsifier, and thus formed particles with mean diameter(16±s 3) nm after diluting with saline.The acute hypersensivitity of self microemulsion was more less than that of in guinea pig.The mean retention times (MRT) were 2.52 h for paclitaxel injection and 3.89 h for self microemulsion. After all, self microemulsion elongated drug retention time in rats. CONCLUSION: Paclitaxel self microemulsion prepared with optimization prescription is safe and stable with remarkably decreasing the hypersensitivity in comparing with paclitaxel injection.