Preparation Of Self-emulsifying Adriamycin-loaded Nanoparticles

As a new kind of drug carrier,nanoparticles were thought to have the broad application prospect.But this carrier was also faced some problems such as preparation or biological safety In the study,self-emulsifying nanoparticles drug delivery system was prepared at room temperature while stirring,which avoids using potential toxic solvent or components.The anticancer drug adriamycin?DOX?was chosen as a model drug and DOX-loaded nanoparticles were prepared by the lecithin,alginate,CaCl₂ and chitosan.The content of doxorubicin was determined by UV spectrophotometric,and then research precision and recovery rate.The results indicate that RSD of the precision of high,medium and low concentrations was 0.90%,0.42%and 0.33%in day,RSD of the precision was 1.12%,0.78%and 0.57%in different days.RSD of recovery was 1.41%.The entrapment efficiency and drug loading capacity as evaluation index of single factor to screening comosed of prescription adriamycin nanoparticles,then through the orthogonal expetiment to optimize the prescription,and ultimately determine the prescription of DOX-loaded nanoparticles was the concentration of adriamycin 1.0mg/mL,the concentration of alginate was 0.63 mg/mL,the concentration of CaCl₂ was 2mg/mL,the amount of chitosan was 30mL.The encapsulation efficiency was 85.5±1.5%,the drug loading capacity was 5.15±0.65%.Self emulsifying time,Particle morphology,particle size was determined in this paper,and to study release of DOX nanoparticles in vitro.The shape of nanoparticles was oval or spherical,uniform distribution,size of nanoparticles was 587nm,and the cumulated release was above 90%in 144 hours.It was unconvenient that liquid preparations of nanoparticles was easy to change their shapes,particle size increased,encapsulation efficiency decreased in the storage,transport and clinical application.Therefore,liquid preparations of Adriamycin nanoparticles could form the solid dry powder by freeze-drying to improve the stability of the preparation.5%sucrose was chosed as lyoprotectant for get the freeze-dried,the lyophilized had more full shape,color uniformity,no piebald and good dispersion.After reconstituted lyophilized powder,we do a quality evaluation.The study showed that the average particle size was 654nm.The particles were round,smooth,encapsulation efficiency was 81%,loading capacity was 4.2%.Because of DOX had good therapeutic effect to hepatic cance,hepatic cancer cell line HepG2 was choiced as the model,MTT assay was used to investigate the inhibition effect of DOX-loaded nanoparticles to cells.The results showed that inhibition effect was showed time-dependent and concentration-dependents.