The Study Of Osthole Niosome

Noisome was a novel microparticle drug delivery system similar to liposome. The synthetic non-ion surfactants were used as film material in noisome alternatives to phospholipids in liposome, the synthetic non-ion surfactants in water could be self-assembled into the vehicles with molecular bilayer structure. Fat-soluble and water-soluble drugs can be entrapped in noisome, it can delay in-vivo release. Niosomes could modify drugs in vivo disposition, they were mainly licked up by the reticulo-endothelial system in body, they can enhance the drug targeted action for the organs such as he liver, the spleen, the lung and the marrow organizes, improve the drug therapeutic effect and reduce the toxic action.Niosomes were widely used as the anticancer drug delivery systems.We developed intravenous niosome of osthole in this study, We investigated the effect of preparation methods, formulae and so on factors on the encapsulation efficiency, studied its hemolytic,leakage rate and pharmacokinetic characteristics in rats.Osthole niosomes were prepared by film dispersion-ultrasonic method, after screened by orthogonal experimental design, the optimized formula was drugs: span-60=1:10(weight ration), cholesterol: span-60 =1: 4 (weight ratio), Tween-80: span-60 =1:2(weight ratio), the pH is 7.4. The optimized preparation: hydration temperature was 60℃,hydration time was 90min,sonication intensity was 300W,sonication time was 8min。The content determination was conducted by HPLC. Glucan gel column chromatography was used to determine the encapsulation efficiency of osthole niosome. Through the transmission electron microscopy, the form of niosome was observed. Results showed that the niosome was intact spherical or oval-shaped ball vesicle, the mean particle diameter was 336nm.After comparing the phenomena of test tubes with negative and positive control, osthole niosomes were found not to cause hemolysis in-vitro. Niosomes were preserved at room temperature and 4℃for ten days respectively ,determine the encapsulation efficiency, leakage rates were 7.4%,2.6% separately, the results showed that the better storage for niosomes temperature is 4℃.In vitro release behavior of osthole niosome was studied by bulk equilibrium dialysis method. The release studies were performed at a fixed temperature 37±0.5℃under stirring(50 r.min),0.5% tween-80 with PBS was used as release medium.Osthole niosome exhibited a certain delayed release profile.The pharmacokinetic characteristics of osthole niosomes in rats were investigated compared with that of osthole solution, and the data were calculated by means of 3p97. According to compartment-model fitting results, osthole niosomes and osthole solution were both fitted with two compartment-model with a weight of 1. T1/2βof osthole niosomes and solution was 74.68±4.35 min and 21.90±3.24min, and the clearance rate was 0.05±0.02ml·min-1 and 0.10±0.04ml·min-1. As the results calculated according to statistical moment theory; AUC of osthole niosomes and solution was 77.37±7.47μg·min·ml-1 and 40.34±6.75μg·min·ml-1 respectively, and MRT was 51.38±4.13min and 26.50±5.14min. Many pharmacokinetic parameters showed significant difference(P<0.05).