Preparation Of Paclitaxel And 5-fluorouracil Multi-drug-loaded System

Purposes:1.Sodiumalginateandchitosan,whicharehuman polysaccharide-absorbable polymers,have better biological advantages than other materials for making sustained-release drugs.In this experiment,they were used to prepare multi-layer drug-loading Microspheres,and its particle size,surface structure and other tests.2.Paclitaxel,5-fluorouracil is a clinical head and neck squamous cell carcinoma,ovarian cancer and other diseases of chemotherapy first-line medication.In this experiment,the two drugs were encapsulated in multi-layer microspheres,and their drug loading and sustained release were studied and tested.Methods:1.Preparation of multi-layered chitosan and sodium alginate microspheres,respectively,under light and electron microscopy to observe the size and surface morphology.2.The microspheres were prepared according to the method of preparing blank microspheres,and the drug-loaded paclitaxel and5-fluorouracil were encapsulated.The size and surface morphology of the microspheres were observed under light microscope and electron microscope respectively.3.Adjust the mobile phase gradient and absorption wavelength gradient to determine the most appropriate HPLC conditions.4.The prepared microspheres placed in a simulated body fluid environment,the supernatant was removed at a specified time,using high performance liquid chromatography were detected drug loading and entrapment efficiency.Result:1.Microspheres are spherical or ellipsoid shape,uniform size,non-adhesion,electron microscopy microscopic surface was reticular structure.The mean diameter of 100 microspheres was?815.93±15.47??m.2.The preparation of drug-loaded microspheres and blank microspheres similar shape,are spherical or ellipsoidal,uniform size,non-adhesion,electron microscopy microscopic surface was reticular structure.The mean diameter of 100 microspheres was?880.43±17.35??m.3.HPLC conditions:Column Acclaim110 C₁₈?250mm*4.6mm,5mm?,flow rate:1.0ml/min;column temperature:35?;injection volume:20?l.Get a suitable mobile phase of methanol and water gradient,detection wavelength gradient.The retention time of 5-Fluorouracil was about 4min,the retention time of paclitaxel was about 14min,and the two reagent peaks showed a good baseline separation from each other and between the reagent peak and the solvent peak.4.The drug loading of 4.5-fluorouracil was?0.29±0.04?%and the entrapment efficiency was?0.3±0.11?%.The drug loading of paclitaxel was?9.27±0.42?%and the entrapment efficiency was?87.25±1.84?%.Conclusion:1.successfully prepared sodium alginate-chitosan multi-layered microspheres,microspheres uniform shape,non-adhesion,uniform particle size,preparation method is good reproducibility.2.High performance liquid chromatography can detect both paclitaxel and 5-fluorouracil,and both drugs achieve good baseline separation3.Sodium alginate-chitosan microspheres successfully packaged paclitaxel and 5-fluorouracil,and the slow release of drugs.