表柔比星固体脂质纳米粒的制备及透黏膜行为  

Preparation and its permeation behavior of epirubicin solid lipid nanoparticles

作　　者：赵宁[1] 李伟泽[1] 付丽娜[1] 王小宁[1] 马秀 任菲菲 ZHAO Ning;LI Weize;FU Lina;WANG Xiaoning;MA Xiu;REN Feifei(Xi′an Medical University,School of Pharmacy,Xi′an 710021,China)

机构地区：[1]西安医学院药学院,陕西西安710021

出　　处：《化工科技》2022年第1期15-21,共7页Science & Technology in Chemical Industry

基　　金：国家自然科学-青年基金项目(82004075);陕西省教育厅自然科学基金项目(19JK0759);陕西省科技厅项目(2020JM-610);陕西高校青年创新团队建设项目(陕教[2019]90号);西安医学院国家自然科学基金培育项目(2017GJFY10);西安医学院药学省级重点学科建设项目(2016YXXK07,2016YXXK20)。

摘　　要：制备表柔比星固体脂质纳米粒(EPI-SLNs),并考察其体外释放、透黏膜行为。采用复乳法制备EPI-SLNs,并以包封率为评价指标优化其处方及工艺;采用平衡透析法研究EPI-SLNs的体外释药行为;立式扩散池法考察其透黏膜行为。结果表明,在m(表柔比星)=1 mg、m(单硬脂酸甘油酯)=5 mg、m(大豆磷脂)=3.5 mg,V(油相)∶V(内水相)=5,初乳涡旋为30 s、初乳超声为40 s、复乳超声为60 s的条件下,所得EPI-SLNs呈橘红色、有光泽,平均粒径为148.6 nm,电位为-30.8 mV,包封率为72.4%;体外释药过程中,t=8 h累积释放度达65.02%;透黏膜实验中,t=8、12、36 h,EPI-SLNs的黏膜累计透过百分率分别为48.4%、55.12%、62.08%,为水溶液的2、1.96、1.79倍;t>36 h,EPI-SLNs的黏膜滞留百分量为13.84%,是EPI水溶液的0.504倍。表明EPI-SLNs不仅具有显著的缓释行为,且具有更好的黏膜透过性。Epirubicin solid lipid nanoparticles(EPI-SLNs)were prepared and their in vitro release and mucosal penetration behaviors were investigated.EPI-SLNs was prepared by double emulsion method,and its formulation and process were optimized with encapsulation rate as evaluation index.Equilibrium dialysis was used to study the drug release behavior of EPI-SLNS in vitro.The permeable membrane behavior was investigated by vertical diffusion cell method.Its transmucosal behavior was investigated by vertical diffusion method,and then calculate the Mucosal retention.The results showed that EPI-SLNs with good performance could be prepared when the formula was epirubicin 1 mg,Monostearin 5 mg,Soybean lecithin 3.5 mg,the volume ratio of oil phase to internal water phase is 5,and under the conditions of 30 s colostrum vortex time,40 s colostrum ultrasound time and 60 s multiple emulsion ultrasound time,the EPI-SLNs was orange-red in appearance,with an average particle size of 148.6 nm,potential-30.8 mV and entrapment efficiency of 72.4%.The in vitro drug release showed that the EPI-SLNs had significant sustained release effect,when 8 h the release rate was 65.02%.The results showed that the cumulative penetration rates of EPI-SLNs at 8 h,12 h and 36 h were 48.4%,55.12%and 62.08%,respectively,which were 2,1.96 and 1.79 times of those in aqueous solution.36 hours later,EPI-SLNs had 13.84%Mucosal retention,which was 0.504 times of EPI aqueous solution.The results showed that EPI-SLNs not only had significant sustained-release behavior,but also had better mucosal permeability.

关 键 词：表柔比星 固体脂质纳米粒 复乳法 体外释药 透黏膜 

分 类 号：R943[医药卫生—药剂学]