摘要
目的对绿原酸(CA)脂质体进行处方筛选、体外释放实验,并考察其对乳腺癌MCF-7细胞的增殖抑制作用。方法筛选制备CA脂质体的方法,并以磷脂比(因素A)、药脂比(因素B)、胎牛血清的p H(因素C)为单因素考察指标,通过正交试验筛选最优处方。采用透析袋法进行体外释放试验。采用噻唑蓝试验考察CA和CA脂质体对MCF-7细胞的增殖抑制作用。结果采用薄膜分散法制备的CA脂质体优于乙醇注入法和逆向蒸发法,平均粒径为225.5 nm,多分散系数(PDI)值为0.21。三因素对包封率的影响程度为A>B>C,最优处方为A_2B_2C_1,即A为4∶1,B为1∶20,C为6.6。CA在最初0.5 h存在突释现象,释放已达到66.90%;而CA脂质体无明显突释现象,8 h累计释放为49.78%;48 h时,CA脂质体累计释放度为85.63%。CA脂质体缓释作用优于游离药物,差异有统计学意义(P<0.05)。结论 CA脂质体具有一定的缓释作用,且对MCF-7细胞的增殖抑制作用明显强于CA。
Objective To conduct the formula screening,in vitro releasing test of chlorogenic acid（CA） liposomes and to investigate its inhibiting effect on breast cancer MCF-7 cell proliferation. Methods The CA liposome preparation method was screened. With phospholipid ratio（factor A）,drug to lipid ratio（factor B） and fetal calf serum p H（factor C） as the single factor investigation indicators,the optimal formula was screened by the orthogonal experiment. The in vitro release test was conducted by adopting dialysis bag method. The inhibiting effect of CA and CA liposomes on MCF-7 cell proliferation was explored by MTT assays. Results Adopting the thin film dispersion method for preparing CA liposomes was superior to the ethanol injection method and reverse evaporating method. The average grain diameter was 225.5 nm,the polydispersity index（PDI） was 0.21.The influence degree of 3 factors on encapsulation rate was A〉B〉C,the optimal formula was A_2B_2C_1,i.e.,A was 4∶1,B was 1∶20 and C was 6.6.The sudden release phenomenon in CA existed at initial 0.5 h,the release reached 66.90%;but CA liposomes had no obvious sudden release phenomenon. The 8 h accumulative release was 49.78%;at 48 h,the accumulative release degree of CA liposomes was 85.63%.The sustained release effect of CA liposomes was superior to that of free drug,the difference was statistically significant（P〈0.05）. Conclusion CA liposomes have a certain sustained-release effect,moreover their inhibiting effect on MCF-7 cell proliferation is significantly stronger than that of CA.
作者
赵玉玺
梅雪
陈珍
杨琴
魏莹
陈钏
Zhao Yuxi Mei Xue Chen Zhen Yang Qin Wei Ying Chen Chuan(Institute of Medicine, School of Pharmacy, North Sichuan Medical University, Nanchong, Sichuan 637000, Chin)
出处
《现代医药卫生》
2017年第15期2263-2265,2269,共4页
Journal of Modern Medicine & Health
关键词
绿原酸
脂质体
乳腺肿瘤
细胞增殖
因素分析
Chlorogenic acid
Liposomes
Breast neoplasms
Cell proliferation
Factor analysis
