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In this study,using a spontaneous emulsification/solvent extraction method,BCNU-loaded PLA nanoparticles (NPs) with small particle size and narrow size distribution have been acquired. The particle size of the NPs ranged from 40~60 nm and 100~200 nm according to different requirements. SEM and TEM showed that the particle size considerably decreases with increasing emulsification concentration and decreasing PLA concentration and ratio of oil to water. The highest drug loading ratio and drug encapsulation efficiency of NPs were 5.63% and 33.45%. The results demonstrated that decrease of initial BCNU content resulted in a noticeably increased encapsulation yield. A thorough study in vitro showed that the drug could be steadily released from NPs for one week. In addition,drug-loaded NPs had higher antitumor activity,compared with free BCNU,and sustained drug release characteristics as well.
In this study, using a spontaneous emulsification / solvent extraction method, BCNU-loaded PLA nanoparticles (NPs) with small particle size and narrow size distribution have been acquired. The particle size of the NPs ranged from 40-60 nm and 100-200 nm according to different requirements. SEM and TEM showed that the particle size significant decreases decreases with increasing emulsification concentration and decreasing PLA concentration and ratio of oil to water. The highest drug loading ratio and drug encapsulation efficiency of NPs were 5.63% and 33.45%. The results demonstrated that decrease of initially BCNU content resulted in a noticeably increased encapsulation yield. A thorough study in vitro showed that the drug could be steadily released from NPs for one week. In addition, drug-loaded NPs had higher antitumor activity, compared with free BCNU , and sustained drug release characteristics as well.