Objective： To establish an albendazole-loaded self-microemulsifying drug delivery system (ABZ-SMEDDS) to improve the solubility and oral bioavailability of the water poorly soluble drug. Methods： The composition of the self-microemulsion prescription was optimized by the establishment of pseudo-triphasic diagrams, then the particle size, drug loading, encapsulation rate, and micromorphology were determined. The in vitro drug release and cytotoxicity and cellular uptake were investigated on a Caco-2 cell model, and finally, the oral bioavailability of ABZ-SMEDDS in rats was investigated. Results： The optimal prescription composition of ABZ-SMEDDS is clove oil, polyoxyethylene hydrogenated castor oil RH40 and polyethylene glycol 400 in a mass ratio of 0.20∶0.64∶0.16. The particle size of ABZ-SMEDDS was (52.14±1.82)nm with a polydispersity index of 0.084±0.006. The drug loading and encapsulation efficiency were (36.60±1.20)mg/g and (98.12±2.2)%, respectively. The results of in vitro release and cell experiments showed that the dissolution rate of ABZ-SMEDDS in different dissolution media were greatly improved compared with ABZ, and it can promote the transmembrane absorption of drugs. Pharmacokinetic results in vivo showed that the relative oral bioavailability of ABZ-SMEDDS in rats was increased to 151.95% compared with the free drug. Conclusion： SMEDDS could be a potential carrier for the enhancement of drug dissolution and oral bioavailability of poorly water soluble drugs.
［Key words］albendazole; selfmicroemulsion; dissolution in vitro; cellular uptake; oral bioavailability