Preparation Of Tamoxifen Microcapsulesand Microspheres And Their Applications On Textiles

Tamoxifen has been the endocrine therapy of breast cancer since the advent of the 1970s.It was approved by FDA in October 1998 for preventing women at high risk from breast cancer.It was the first and only allowed to be used to prevent breast cancer drug so far.But there are many limitations,such as short drug-delivery time, strong stomach irritation,and so on.The purpose of this study is to prepare tamoxifen microcapsules and microspheres which have slow-releasing effect,and to obtain a newly drug tamoxifen formulations in order to improve the tamoxifen drug tablets' shortcomings such as short time release,stimulating the stomach.Then,tamoxifen microcapsules and microspheres were applied onto textile,and we designed and fabricated a medicated system that potentially could be applied within a transdermal drug delivery system and so act in a system for the treatment of breast cancer.The microcapsules were prepared using a simple coacervation and complex coacervation procedure.The morphology,particle size,drug loading capacity and in vitro release characteristics of the drug microcapsules were optimized.The properties of the microcapsules such as particle size,size distribution,surface patterns,in vitro release and so on were tested.The results showed that the microcapsules obtained for particle size,distribution,stability,drug loading and encapsulation efficiency were more improved and more effective for sustained-release.Tamoxifen microspheres were prepared using solvent evaporation method.The solvent,PLGA type and some other factors were optimized.The properties of the microcapsules such as particle size,size distribution,surface patterns,in vitro release etc.were tested.The results showed that the microspheres have small particle size, good distribution,high drug loading and encapsulation efficiency and good sustained-release effect.Tamoxifen microcapsules and microspheres were applied to fabric using padding, dipping,and coating methods.The amount of microcapsules and microspheres,the amount of adhesive,temperature etc.were investigated.The washing fastness and air permeability of the drug loading fabric were also measured.The results showed that the fabric prepared by Coating method containing the most tamoxifen microcapsules and microspheres,better wash fastness,but poorer permeability compared with the other two methods.UV was used to determine the drug loading and encapsulation efficiency of tamoxifen microcapsules and microspheres.Tamoxifen microcapsules and microspheres were identified by IR and SEM.In vitro release properties and release mechanism were studied by dissolution apparatus and UV.The curve of the percentage of the cumulative release versus time was made.The results showed that, even though burst release was observed at early stage,the tamoxifen drug delivery system developed in this study exhibited good performance in vitro release profiles, improved the performance of tamoxifen to some extent.