Functional Preparation And Application Of Multiphase Drug-loaded Microspheres

The deterioration of the ecological environment makes the incidence of cancer rapid rise in recent years.Paclitaxel as a broad-spectrum anticancer drugs in the treatment of tumors used more,but its preparation in clinical use in the following problems:(1)Cremophor EL as a solvent will produce serious allergic reactions and toxic side effects;(2)Liposomal formulations poor storage stability;(3)human serum albumin binding formulations without active targeting;(4)a single function.In view of the problems of paclitaxel,there is an urgent need to develop a novel multifunctional and safe drug carrier.The purpose of this study was to develop a functional multiphase drug-loaded microsphere with the functions of magnetic targeting,fluorescence monitoring and drug delivery.In this study,functional multiphase drug-loaded microspheres were prepared by electrohydrodynamic(EHD)co-jetting technique.The research scheme is as follows:(1)The feasibility of the multiphase structure was confirmed by LSCM observation,and the optimized process parameters were obtained.The microspheres were prepared by electrostatic co-jet technique.(2)Morphology of functional multiphase drug loaded microspheres was characterized by SEM and LSCM.Magnetic properties were analyzed by VSM and magnetometer.The paclitaxel was analyzed by FT-IR,XRD and DSC.(3)The in vitro assay of paclitaxel was established by HPLC.The drug loading and entrapment efficiency of functional multiphase drug loaded microspheres were studied.The cumulative release rate of paclitaxel in different release media was explored.(4)The biocompatibility and antitumor effect of functional multiphase drug loaded microspheres were evaluated using mouse embryonic fibroblasts and human breast cancer cells.The results showed that the functional spherical microspheres were smooth,the size of the microspheres was uniform and the size distribution of the microspheres was mainly between 3-5?m.The morphology of the microspheres showed no change before and after drug loading Stability is better.The magnetic properties of the microspheres are good and under the action of the magnet,the microspheres can be observed in the fluorescence and macroscopic environment.Microspheres were loaded with paclitaxel and the crystal form changed.The drug loading and entrapment efficiency of the microspheres were improved,and the sustained-release effect was good.The biocompatibility and anti-cancer effect were also obtained.The functionalized multiphase drug-loaded microspheres developed in this study can solve the shortcomings of the existing paclitaxel preparations.Good biocompatibility of the microspheres provides a basis for clinical application and provides new ideas and methods for the development of pharmaceutical preparations.